Information on EC 1.14.19.1 - stearoyl-CoA 9-desaturase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY
1.14.19.1
-
RECOMMENDED NAME
GeneOntology No.
stearoyl-CoA 9-desaturase
-
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
An iron protein. The rat liver enzyme is an enzyme system involving cytochrome b5 and EC 1.6.2.2, cytochrome-b5 reductase. Formerly EC 1.14.99.5; arginyl and tyrosyl residues expected in the active site of enzyme
-
-
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
the reducing equivalents required for the desaturation site seem to be supplied from NADPH via cytochrome b5 as electron carrier
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
multienzyme, insertion of a double bond in 9,10 position
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
cytochrome b5, cytochrome b5 reductase and lipid and/or detergent are needed for all assays. A cis-hydrogen abstraction mechanism is involved in desaturation
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
electron flow from NADH to cytochrome b5, via cytochrome b5 reductase. Different types of acyl-CoA desaturation show immunological differences
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
incorporation of fatty acid into phospholipid. Enzyme may contain an essential thiol group. Endogenous saturated phospholipid is desaturated rapidly in all experiments in contrast with exogenous saturated phospholipid, which generally is not desaturated
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
presence of an unusual microsomal electron transport system associated with the desaturase
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
significant amounts of DELTA8-isomers are present
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
introduction of double bonds at fixed positions from the carboxyl group of the fatty acid. D-hydrogen atoms are removed during desaturation. Mixed-function oxidase, acting via hydroxy acid intermediates. Acetyl-CoA desaturase, carboxylase and fatty acid synthetase are all controlled together as a unit and influenced by dietary components
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
introduction of double bond at position 9
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
presence of two desaturase genes, isomers CDS1 and CDS2. Cooling treatment of carp causes significant changes to the activity of the DELTA9-desaturase. Modest cooling of carp shows an increase in acticity without any increase in the amount of desaturase protein, suggesting the activation of the pre-existing inactive latent enzyme, possibly by a post-translational mechanism
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
the synthesis is transcriptionally regulated by fat-free diet and sterols. Cholesterol-supplemented media as well as the transient transfection induces the expression of stearoyl-CoA desaturase RNA
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
it is suggested that in HepG2 cells the trans-10,cis-12 conjugated linoleic acid isomer regulates human desaturase activity mainly by a posttranslational mechanism
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
isolation of a third fatty acid DELTA9-desaturase. Higher activity with longer chain fatty acid substrates. Desaturase expression is induced significantly by increasing the ratio of carbon to nitrogen
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
regioselectivity, substrate specificity, probably extra-plastidal
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
increase of activity induced by cold is preceded by the activation of latent desaturase, probably by a posttranslational mechanism. Amounts of desaturase transcript are increased as a result of cold-induced gene transcription
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
cold exposure leads to an induced activity, in vivo cooling causes an activity induction of up to 15 to 30fold. Increase of desaturase synthesis by means of activated gene transcription. Transfer of cells to 10C causes a smaller increase in activity compared to cells maintained at 30C
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
the possible mechanism would be that dioxygen has to bind to both irons for effective two-electron transfer to the half-occupied antibonding pi orbitals of dioxygen to give a peroxide level intermediate
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
existence of three highly homologous isoforms: SCD1, SCD2 and SCD3 which show different substrate specificities, here SCD1 is mainly analysed
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
SSI2 gene encodes a member of a family of soluble fatty acid desaturases
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
cold exposure leads to an induced activity, in vivo cooling causes an activity induction of up to 15 to 30fold. Increase of desaturase synthesis by means of activated gene transcription. Transfer of cells to 10C causes a smaller increase in activity compared to cells maintained at 30C; presence of two desaturase genes, isomers CDS1 and CDS2. Cooling treatment of carp causes significant changes to the activity of the DELTA9-desaturase. Modest cooling of carp shows an increase in acticity without any increase in the amount of desaturase protein, suggesting the activation of the pre-existing inactive latent enzyme, possibly by a post-translational mechanism
Cyprinus carpio L.
-
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
isolation of a third fatty acid DELTA9-desaturase. Higher activity with longer chain fatty acid substrates. Desaturase expression is induced significantly by increasing the ratio of carbon to nitrogen
Mortierella alpina CBS 528.72
-
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
cytochrome b5, cytochrome b5 reductase and lipid and/or detergent are needed for all assays. A cis-hydrogen abstraction mechanism is involved in desaturation
Rattus norvegicus Long-Evans
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
oxidation
-
-
-
-
redox reaction
-
-
-
-
reduction
-
-
-
-
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
oleate biosynthesis II (animals and fungi)
-
-
sorgoleone biosynthesis
-
-
Biosynthesis of unsaturated fatty acids
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-
SYSTEMATIC NAME
IUBMB Comments
stearoyl-CoA,ferrocytochrome-b5:oxygen oxidoreductase (9,10-dehydrogenating)
An iron protein. The rat liver enzyme is an enzyme system involving cytochrome b5 and EC 1.6.2.2, cytochrome-b5 reductase. The ferricytochrome b5 produced is reduced by NADH and cytochrome-b5 reductase (EC 1.6.2.2).
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ACOD4
-
-
acyl coenzyme A desaturase
-
-
-
-
acyl-CoA desaturase
-
-
-
-
acyl-CoA desaturase
-
-
delta-9 desaturase
-
-
delta-9 desaturase
-
-
DELTA9 desaturase
-
-
DELTA9 desaturase
-
-
DELTA9 desaturase
-
-
DELTA9 desaturase
-
-
DELTA9 fatty acid desaturase
-
-
DELTA9 fatty acid desaturase
Pseudoalteromonas sp. MLY15
-
-
-
DELTA9 terminal desaturase
-
-
DELTA9-acyl CoA desaturase
-
-
-
-
DELTA9-desaturase
-
-
-
-
DELTA9-desaturase
-
-
DELTA9-fatty-acid desaturase
-
desaturase 9
-
-
Dpu-DELTA9-KPSE
-
EC 1.14.99.5
-
-
formerly
-
eicosatrienoyl-CoA desaturase
-
-
-
-
FAD9
Pseudoalteromonas sp. MLY15
-
-
-
fatty acid 9-desaturase
-
-
-
-
fatty acid DELTA9-desaturase
-
-
-
-
fatty acid desaturase
-
-
-
-
fatty acid desaturase
-
-
fatty acyl CoA DELTA9-desaturase
-
-
-
-
fatty acyl DELTA9-desaturase
-
-
-
-
fatty acyl-CoA desaturase
-
-
-
-
hSCD1
-
-
long-chain fatty acid DELTA9-desaturase
-
-
-
-
membrane-bound stearoyl-CoA DELTA9 desaturase
-
-
membrane-bound stearoyl-CoA DELTA9 desaturase
-
-
-
NPVE desaturase
-
-
palmitoyl CoA desaturase
-
-
-
-
palmitoyl-CoA desaturase
-
-
-
-
SCD
Trypanosoma brucei Lister 427
-
-
-
SCD-1
-
-
SCD-1
-
isoform
SCD-2
-
isoform
SCD-3
-
isoform
SCD-4
-
isoform
SCD1
-
-
SCD1
Mus musculus Rj:NMRI
-
-
SCD1
-
-
SCD2
-
-
SCD2
Mus musculus Rj:NMRI
-
-
SCD3
Mus musculus Rj:NMRI
-
-
SCD4
-
-
stearoyl CoA desaturase
-
-
stearoyl coenzyme A desaturase
-
-
-
-
stearoyl coenzyme-A desaturase 1
-
-
stearoyl-ACP DELTA9 desaturase
-
-
stearoyl-CoA (DELTA8) desaturase
-
-
-
-
stearoyl-CoA desaturase
-
-
-
-
stearoyl-CoA desaturase
-
-
stearoyl-CoA desaturase
-
stearoyl-CoA desaturase
-
stearoyl-CoA desaturase
-
-
stearoyl-CoA desaturase
-
-
stearoyl-CoA desaturase
-
-
-
stearoyl-CoA desaturase
-
stearoyl-CoA desaturase
-
stearoyl-CoA desaturase
-
-
stearoyl-CoA desaturase
-
-
stearoyl-CoA desaturase
Trypanosoma brucei Lister 427
-
-
-
stearoyl-CoA desaturase 1
-
-
stearoyl-CoA desaturase 1
-
stearoyl-CoA desaturase 1
-
-
stearoyl-CoA desaturase 2
-
-
stearoyl-CoA desaturase 2
-
stearoyl-CoA desaturase enzyme-1
-
-
stearoyl-CoA desaturase-1
-
stearoyl-CoA desaturase-1
-
-
stearoyl-CoA desaturase-5
-
-
stearoyl-CoA desaturase1
-
-
stearoyl-CoA desaturase2
-
-
stearoyl-coenzyme A desaturase
-
-
stearoyl-coenzyme A desaturase-1
-
-
stearyl coenzyme A desaturase
-
-
-
-
stearyl-CoA desaturase
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
9014-34-0
-
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
isoform ADS1, ADS2
-
-
Manually annotated by BRENDA team
; Angus steer
-
-
Manually annotated by BRENDA team
; short- and long-fed Angus and Wagyu steers with corn-based or hay-based diets
-
-
Manually annotated by BRENDA team
cow
-
-
Manually annotated by BRENDA team
higher enzymic acitivity in Jersey-sired cattle than in Limousin-sired cattle, positive relationship between adipose tissue beta-carotene and desaturation
-
-
Manually annotated by BRENDA team
isozyme SCD1; isozyme SCD1
UniProt
Manually annotated by BRENDA team
isozyme SCD5; isozyme SCD5
UniProt
Manually annotated by BRENDA team
steers
UniProt
Manually annotated by BRENDA team
milk fish, enzyme activity increases significantly in the beginning of cold acclimation, peaks at day 4 and then decreases constantly. Change of enzyme activity parllels the change of DELTA9 desaturation in the animal
-
-
Manually annotated by BRENDA team
grass carp, enzyme activity increases gradually in the first week of cold acclimation, increases dramatically afterward and the maintains a very high level. Change of enzyme activity parllels the change of DELTA9 desaturation in the animal
-
-
Manually annotated by BRENDA team
transient upregulation of isoform Cps2 during first days of cold acclimation, no substantial response of isoform activity to diet of saturated fatty acids
SwissProt
Manually annotated by BRENDA team
Cyprinus carpio L.
L.
-
-
Manually annotated by BRENDA team
f. sp. lycopersici
-
-
Manually annotated by BRENDA team
brown dwarf laying hen
-
-
Manually annotated by BRENDA team
embryo
-
-
Manually annotated by BRENDA team
L., sunflower
-
-
Manually annotated by BRENDA team
hSCD1 cloned from a human liver cDNA library
-
-
Manually annotated by BRENDA team
hSCD5 cloned from a human brain cDNA library
SwissProt
Manually annotated by BRENDA team
male humans
-
-
Manually annotated by BRENDA team
gene SCD1; male hamsters, isozyme SCD1
UniProt
Manually annotated by BRENDA team
gene SCD2; male hamsters, isozyme SCD2
UniProt
Manually annotated by BRENDA team
gene SCD3 or FAR-17c; male hamsters, isozyme SCD3
UniProt
Manually annotated by BRENDA team
male Golden Syrian Hamsters
-
-
Manually annotated by BRENDA team
strain CBS 528.72, ATCC 32222
-
-
Manually annotated by BRENDA team
Mortierella alpina CBS 528.72
strain CBS 528.72, ATCC 32222
-
-
Manually annotated by BRENDA team
129 SvEv wild-type and Sc1-/- mice
-
-
Manually annotated by BRENDA team
C57BL/6J mice
-
-
Manually annotated by BRENDA team
C57Bl/B6 and 129S6/SvEvTac mice
-
-
Manually annotated by BRENDA team
enzyme inhibition by specific antisense oligonucleotide inhibitors, reduction of enzyme expression, reduction of fatty acid synthesis and secretion, increase in fatty acid oxidation
-
-
Manually annotated by BRENDA team
ob/ob mice
-
-
Manually annotated by BRENDA team
ob/ob mice, isoform SCD4, tissue-specific regulation by leptin and dietary factors
SwissProt
Manually annotated by BRENDA team
Rj:NMRI mice
SwissProt
Manually annotated by BRENDA team
Rj:NMRI mice
TrEMBL
Manually annotated by BRENDA team
Mus musculus C57BL/6J
C57BL/6J mice
-
-
Manually annotated by BRENDA team
Mus musculus Rj:NMRI
Rj:NMRI mice
SwissProt
Manually annotated by BRENDA team
Mus musculus Rj:NMRI
Rj:NMRI mice
TrEMBL
Manually annotated by BRENDA team
strain H37Rv, gene rv3229c
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-
Manually annotated by BRENDA team
strain H37Rv, gene rv3229c
-
-
Manually annotated by BRENDA team
white pruce
-
-
Manually annotated by BRENDA team
strain 3D7
UniProt
Manually annotated by BRENDA team
strain MLY15
-
-
Manually annotated by BRENDA team
Pseudoalteromonas sp. MLY15
strain MLY15
-
-
Manually annotated by BRENDA team
Colworth-Wistar, male
-
-
Manually annotated by BRENDA team
insulin-resistent ZDF rats, Zucker diabetic fatty rats
-
-
Manually annotated by BRENDA team
Sprague-Dawley rats
SwissProt
Manually annotated by BRENDA team
Sprague-Dawley, male
-
-
Manually annotated by BRENDA team
Spraque-Dawley rats
-
-
Manually annotated by BRENDA team
Wister, male
-
-
Manually annotated by BRENDA team
Rattus norvegicus Long-Evans
Long-Evans
-
-
Manually annotated by BRENDA team
two isozymes
-
-
Manually annotated by BRENDA team
Trypanosoma brucei Lister 427
-
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
alterations in expression reported in several prevalent metabolic diseases, such as diabetes, obesity and atherosclerosis
malfunction
-
enzyme inhibition by genetic and chemical tools is detrimental for parasite development. The partial ablation of the enzyme inhibits drastically the parasite growth
malfunction
-
the ablation of enzyme activity has an immediate and profound impact on the fatty acid content of cell lipids. Enzyme inhibition alters the epidermal growth factor-dependent signaling mechanism, decreases the mobility of fluid domains in plasma membranes, and reduces EGF-induced proliferation in lung cancer cells
malfunction
-
stearoyl-CoA desaturase 1 deficiency is coupled with an extreme cold sensitivity and significantly increased skin inflammation
malfunction
Trypanosoma brucei Lister 427
-
enzyme inhibition by genetic and chemical tools is detrimental for parasite development. The partial ablation of the enzyme inhibits drastically the parasite growth
-
metabolism
-
SCD is critical in the biosynthesis of triglycerides, cholesterol esters, wax esters, and 1-alkyl-2,3-diacylglycerol
metabolism
sex-pheromone biosynthesis; sex-pheromone biosynthesis; sex-pheromone biosynthesis; sex-pheromone biosynthesis; sex-pheromone biosynthesis
metabolism
-
the enzyme is necessary for proper liver, adipose tissue, and skeletal muscle lipid metabolism
metabolism
-
stearoyl-CoA desaturase 1 is the rate-limiting enzyme in the biosynthesis of monounsaturated fatty acids and a risk factor of diabetes
physiological function
-
SCD-1 knockout mice show reduced body adiposity, increased insulin sensitivity, leanness, increased metabolic rate, and resistance to diet-induced obesity
physiological function
-
absence of stearoyl-CoA desaturase-1 leads to chronic inflammation of the skin and increased susceptibility to atherosclerosis, while also increasing plasma inflammatory markers, but does not promote dextran sulfate sodium-induced acute colitis
physiological function
-
mice lacking Scd1 are protected from obesity and insulin resistance and are characterized by decreased fatty acid synthesis and increased fatty acid oxidation
physiological function
-
Scd1 null mice are more susceptible to dextran sulfate sodium treatment than wild type mice, while oleic acid feeding and in vivo SCD1 rescue with SCD1 adenovirus alleviates the dextran sulfate sodium-induced phenotype
physiological function
-
mice with a skin-specific deletion of SCD1 (SKO) have significantly increased energy expenditure, are protected from high fat diet-induced obesity, and display marked sebaceous gland hypoplasia and depletion of sebaceous lipids. SKO mice display severe cold intolerance because of rapid depletion of fuel substrates, including hepatic glycogen, to maintain core body temperature. Unlike mice globally deficient in SCD1, SKO mice have an intact hepatic lipogenic response to acute high carbohydrate feeding
physiological function
-
SCD1 knockout mice on the methionine-choline-deficient diet have decreased steatosis and markedly increased hepatocellular apoptosis, liver injury, and fibrosis compared with the SCD-expressing mice
physiological function
-
key regulator of lipid fatty acid composition
physiological function
-
enzyme expression is important in regulating lipid bilayer fluidity, increasing triglyceride formation, and enabling lipogenesis and may protect against saturated fatty acids-induced lipotoxicity
physiological function
-
the enzyme activity is the most critical determinant of the monounsaturated/saturated fatty acid balance in cancer cells
physiological function
-
skin stearoyl-CoA desaturase 1 regulates skin integrity and energy balance
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
18-fluoro-10-thiaoctadecanoyl-[acyl-carrier protein] + O2 + ferredoxin
?
show the reaction diagram
-
-
-
-
?
ammonium stearate + NADH + O2
?
show the reaction diagram
-
-
-
-
?
myristic acid + NADH + O2 + ATP + CoA
myristoleic acid + NAD+ + H2O + ?
show the reaction diagram
-
reaction in presence of fatty acid-binding proteins with mixing at speeds between 250 and 500 rpm
-
?
myristoyl-CoA + AH2 + O2
?
show the reaction diagram
-
-
-
-
?
myristoyl-CoA + AH2 + O2
?
show the reaction diagram
-
-
-
-
?
myristoyl-CoA + AH2 + O2
?
show the reaction diagram
-
59% activity of the rate with stearoyl-CoA
-
-
?
myristoyl-CoA + NADH + O2
?
show the reaction diagram
-
59% activity of stearoyl-CoA
-
-
?
myristoyl-CoA + NADH + O2
myristoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
N-hydroxy-benzenecarboximidamide + NADH + H+ + O2
benzamidine + NAD+ + H2O
show the reaction diagram
-
-
-
?
nonadecanoate + AH2 + O2
?
show the reaction diagram
-
low activity
-
-
?
nonadecanoyl-CoA + NADH + O2
?
show the reaction diagram
-
-
-
-
?
palmitic acid + AH2 + O2
palmitoleic acid + A + H2O
show the reaction diagram
-
-
-
?
palmitic acid + AH2 + O2
palmitoleic acid + A + H2O
show the reaction diagram
-
-
-
?
palmitic acid + AH2 + O2
palmitoleic acid + A + H2O
show the reaction diagram
Mortierella alpina CBS 528.72
-
-
-
?
palmitic acid + reduced acceptor + O2
palmitoleic acid + acceptor + H2O
show the reaction diagram
-
-
-
?
palmitic acid + reduced acceptor + O2
palmitoleic acid + acceptor + H2O
show the reaction diagram
preferred substrate
-
?
palmitic acid + reduced acceptor + O2
palmitoleic acid + acceptor + H2O
show the reaction diagram
-
isozyme Sls-FL2, preferred substrate
Z-isomer, both isozymes
?
palmitic acid + reduced acceptor + O2
palmitoleic acid + acceptor + H2O
show the reaction diagram
Pseudoalteromonas sp. MLY15
-
-
-
?
palmitoyl-CoA + AH2 + O2
palmitoleoyl-CoA + A
show the reaction diagram
-
-
-
?
palmitoyl-CoA + AH2 + O2
palmitoleoyl-CoA + A
show the reaction diagram
-
-
-
?
palmitoyl-CoA + AH2 + O2
palmitoleoyl-CoA + A
show the reaction diagram
-
62% activity of the rate with stearoyl-CoA
-
?
palmitoyl-CoA + AH2 + O2
palmitoleoyl-CoA + A
show the reaction diagram
Cyprinus carpio L.
-
-
-
?
palmitoyl-CoA + AH2 + O2
palmitoleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + ferrocytochrome b5 + O2
palmitoleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + ferrocytochrome b5 + O2 + 2 H+
palmitoleoyl-CoA + ferricytochrome b5 + 2 H2O
show the reaction diagram
-
a key step in triglyceride synthesis in the fatty acid metabolic network
-
?
palmitoyl-CoA + NAD(P)H + O2
palmitoleate + NAD(P)+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + H+ + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + H+ + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
13% conversion
-
?
palmitoyl-CoA + NADH + H+ + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
main substrate
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
slight activity
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
62% activity of stearoyl-CoA
-
?
palmitoyl-CoA + NADH + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
SCD activity of microsomal fraction
-
?
palmitoyl-CoA + NADPH + O2
?
show the reaction diagram
-
-
-
-
?
palmitoyl-CoA + NADPH + O2
palmitoleoyl-CoA + NADP+ + H2O
show the reaction diagram
-
Angus and American Wagyu steers, corn-fed steers for 8 mo (short-fed) or 16 mo (long-fed), and hay-fed steers fed for 12 mo (short-fed) and 20 mo (long-fed)
-
?
palmitoyl-CoA + NADPH + O2 + H+
palmitoleoyl-CoA + NADP+ + H2O
show the reaction diagram
-
-
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
-
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
-
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
-
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
-
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
maximum activity
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
biosynthesis of unsaturated fatty acid, synthesis of triacylglycerol from oleate
-
-
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
Mortierella alpina CBS 528.72
-
-
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
Cyprinus carpio L.
-
-
-
?
stearate + AH2 + O2
oleoyl-phospholipid + A + H2O
show the reaction diagram
-
-
-
?
stearate + reduced acceptor + O2
oleate + acceptor + H2O
show the reaction diagram
-
-
-
?
stearate + reduced acceptor + O2
oleate + acceptor + H2O
show the reaction diagram
-
-
?
stearate + reduced acceptor + O2
oleate + acceptor + H2O
show the reaction diagram
-
isozyme Sls-FL1, preferred substrate
Z-isomer, both isozymes
?
stearic acid + AH2 + O2
oleic acid + A + H2O
show the reaction diagram
-
-
?
stearic acid + AH2 + O2
oleic acid + A + H2O
show the reaction diagram
the enzyme shows a preference for C18 saturated fatty acids
-
?
stearic acid + reduced acceptor + O2
oleic acid + acceptor + H2O
show the reaction diagram
Pseudoalteromonas sp., Pseudoalteromonas sp. MLY15
-
-
-
?
stearoyl-acyl-carrier protein + AH2 + O2
oleoyl-acyl-carrier protein + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-acyl-carrier protein + AH2 + O2
oleoyl-acyl-carrier protein + A + H2O
show the reaction diagram
-
insertion of a cis double bond between the 9 and 10 position, essential step in fatty acid biosynthesis
-
?
stearoyl-acyl-carrier protein + AH2 + O2
oleoyl-acyl-carrier protein + A + H2O
show the reaction diagram
-
key regulator of fatty acid desaturation of carbons 9 and 10
-
?
stearoyl-CoA + AH2 + H+ + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
also other fatty acyl-CoA substrates
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
oleic acid biosynthesis
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
activity measured via the generation of tritium enriched water from the substrate 9,10-3H-steaoryl-CoA
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
Cyprinus carpio L.
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
Mus musculus C57BL/6J
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
Rattus norvegicus Long-Evans
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
Rattus norvegicus Long-Evans
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + H+ + O2
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
a key step in triglyceride synthesis in the fatty acid metabolic network
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
essential enzyme activity, regulation mechanism, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, deficiency of isozyme SCD1 leads to activation of the metabolic pathways that promote fatty acid beta-oxidation in mice, enzyme regulation in the heart in a hormone-dependent fashion, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, hepatic SCD1 activity may regulate fat accumulation in the liver and possibly protects from insulin resistance in obesity, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, it is also involved in familial combined hyperlipidemia, fatty acid desaturation index, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, key enzyme in lipid metabolism and energy expenditure in mammals, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, which plays an important role in lipid metabolism and body weight control, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
stearoyl-CoA desaturase 2 is uniquely and absolutely required for adipogenesis, SCD2 also controls the maintenance of adipocyte-specific gene expression in fully differentiated 3T3-L1 adipocytes, including the expression of SCD1, polysome profile analysis, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
stearoyl-CoA desaturase converts saturated to monounsaturated fatty acids and is a key enzyme in lipogenesis, elevated levels of endogenous lipogenesis increase the risk of fracture and suggest a role for saturated fat in the pathogenesis of osteoporosis
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
the enzyme catalyzes the desaturation from saturated to monounsaturated fatty acids
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
DesA3 expressed as a fusion with either a C-terminal His6 or c-myc tag has consistently higher activity and stability than native DesA3 having the native C-terminal sequence of LAA
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
essential enzyme activity, regulation mechanism, overview, DesA3 expressed as a fusion with either a C-terminal His6 or c-myc tag has consistently higher activity and stability than native DesA3 having the native C-terminal sequence of LAA
-
?
stearoyl-CoA + NAD(P)H + O2
oleoyl-CoA + NAD(P)+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NAD(P)H + O2
oleoyl-CoA + NAD(P)+ + H2O
show the reaction diagram
-
fatty acid desaturation
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
45% conversion
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
main substrate
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
high activity
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
preferred substrate for SCD1
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
maximal activity
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
terminal component in the enzyme system
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
-
Scd-/- and wild-type mice are fed with 20% high fat diets, fat-free basal mix is supplemented with 20% by weight of tristearin or triolein and 1% by weight corn oil
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
Rattus norvegicus Long-Evans
-
terminal component in the enzyme system
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
Rattus norvegicus Long-Evans
-
-
-
?
stearoyl-CoA + NADPH + H+ + O2
oleoyl-CoA + NADP+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADPH + H+ + O2
oleoyl-CoA + NADP+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADPH + H+ + O2
oleoyl-CoA + NADP+ + H2O
show the reaction diagram
-
-
?
stearoyl-CoA + NADPH + O2
oleoyl-CoA + NADP+ + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + NADPH + O2
oleoyl-CoA + NADP+ + H2O
show the reaction diagram
-
-
-
?
heptadecanoate + AH2 + O2
?
show the reaction diagram
-
low activity
-
-
?
additional information
?
-
-
stearic and palmitic acids are no substrates
-
-
-
additional information
?
-
-
12-19 carbon fatty acyl chains undergo 9,10 desaturation. Dephospho-, deamino- and (1-N6-etheno)-CoA analogs of stearoyl-CoA are poorer substrates than stearoyl-CoA
-
-
-
additional information
?
-
-
preference for 18-carbon versus 16-carbon chain length fatty acids
-
-
-
additional information
?
-
-
glycerolipid such as phosphatidylcholine is involved as an intermediate substrate
-
-
-
additional information
?
-
-
temperature-dependent chain length change is not mediated by a temperature-dependent change in desaturase substrate specificity
-
-
-
additional information
?
-
-
SCD2 and SCD3 preferentially utilize palmitoyl-CoA
-
-
-
additional information
?
-
-
specific for C14-C19 fatty acyl-CoA substrates
-
-
-
additional information
?
-
-
not acyl-CoA as substrate but phospholipid, biosynthesis of unsaturated fatty acids. Possible substrates: acyl-CoA, acyl-acyl-carrier and acyl chains of phospholipids. The substrate in vivo is saturated phospholipid
-
-
-
additional information
?
-
-
rate limiting-step in the cellular synthesis of monounsaturated fatty acids mainly oleate and palmitoleate
-
-
-
additional information
?
-
-
key enzyme in the synthesis of unsaturated fatty acyl-CoAs
-
-
-
additional information
?
-
-
rate-limiting enzyme in the biosynthesis of monounsaturated fatty acids
-
-
-
additional information
?
-
-
incorporation of the first unsaturation bond into saturated fatty acids
-
-
-
additional information
?
-
-
long-chain polyunsaturated fatty acid biosynthetic pathway
-
-
-
additional information
?
-
-
fatty acid binding proteins my regulate the accessibility of fatty acids in the desaturation reaction to the active site
-
-
-
additional information
?
-
-
enzyme activity measured by conversion of 14C-stearic acid to 14C-oleic acid, reverse-phase HPLC
-
-
?
additional information
?
-
-
aging human orbitofrontal cortex includes decreasing of polyunsaturated fatty acid composition associates increases in lipogenic gene expression and stearoyl-CoA desaturase activity, overview
-
-
-
additional information
?
-
-
Angus and Wagyu steers consuming high-roughage diets exhibit large differences in adipose tissue fatty acid composition, but there are no differences in terminal measures of CD activity or gene expression, overview
-
-
-
additional information
?
-
decreased degradation of SCD is responsible for the increase in palmitoyl-CoA chain elongase activity in addition to increased transcription of SCD1 in the rats treated with clofibric acid, overview
-
-
-
additional information
?
-
-
DesA3 is a membrane-bound stearoyl-CoA desaturase that works together with oxidoreductase Rv3230c, encoded by gene rv3230c, to produce oleic acid, an 55 essential constituent of mycobacterial membrane phospholipids and triglycerides
-
-
-
additional information
?
-
-
due to a population-based, longitudinal cohort study of men, the risk of fracture is highest among men with the highest levels of SCD activity index, overview
-
-
-
additional information
?
-
-
inhibition of the enzyme in cholesterol-fed hamsters leads to reduced overall body weight and adipose tissue deposition, while enzyme inhibition in absence of cholesterol does not. Enzyme inhibition induces hypercholesterinemia, overview
-
-
-
additional information
?
-
-
role of SCD1 in fatty acid metabolism in HepG2 cells, the desaturation systems in Hep-G2 cells are strongly compartmentalized, effects of SCD1 inhibition on fatty acid composition in HepG2 cells occur through changes in the dynamics of the fatty acid metabolic network and not through transcriptional regulatory mechanisms, overview
-
-
-
additional information
?
-
the enzyme also produces cis-9, trans-11 conjugated linoleic acid and palmitoleoyl-CoA
-
-
-
additional information
?
-
-
the enzyme reacts with oxidoreductase Rv3230c to produce oleic acid
-
-
-
additional information
?
-
heterologous expression in yeast shows that Dpu-DELTA9-KPSE produces E9 mono-unsaturated fatty acids of various chain lengths. When provided with the (7Z)-tetradec-7-enoate, it forms the (7Z,9E)-tetradec-7,9-dienoate unsaturated fatty acids, another biosynthetic intermediate that can be chain-shortened to (5Z,7Z)-dodeca-5,7-dienoate
-
-
-
additional information
?
-
Mortierella alpina CBS 528.72
-
long-chain polyunsaturated fatty acid biosynthetic pathway
-
-
-
additional information
?
-
-
DesA3 is a membrane-bound stearoyl-CoA desaturase that works together with oxidoreductase Rv3230c, encoded by gene rv3230c, to produce oleic acid, an 55 essential constituent of mycobacterial membrane phospholipids and triglycerides, the enzyme reacts with oxidoreductase Rv3230c to produce oleic acid
-
-
-
additional information
?
-
Rattus norvegicus Long-Evans
-
12-19 carbon fatty acyl chains undergo 9,10 desaturation. Dephospho-, deamino- and (1-N6-etheno)-CoA analogs of stearoyl-CoA are poorer substrates than stearoyl-CoA
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
palmitoyl-CoA + AH2 + O2
palmitoleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
palmitoyl-CoA + ferrocytochrome b5 + O2 + 2 H+
palmitoleoyl-CoA + ferricytochrome b5 + 2 H2O
show the reaction diagram
-
a key step in triglyceride synthesis in the fatty acid metabolic network
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
-
-
?
stearate + AH2 + O2
oleate + A + H2O
show the reaction diagram
-
biosynthesis of unsaturated fatty acid, synthesis of triacylglycerol from oleate
-
-
stearoyl-acyl-carrier protein + AH2 + O2
oleoyl-acyl-carrier protein + A + H2O
show the reaction diagram
-
insertion of a cis double bond between the 9 and 10 position, essential step in fatty acid biosynthesis
-
?
stearoyl-acyl-carrier protein + AH2 + O2
oleoyl-acyl-carrier protein + A + H2O
show the reaction diagram
-
key regulator of fatty acid desaturation of carbons 9 and 10
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
also other fatty acyl-CoA substrates
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
oleic acid biosynthesis
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
Rattus norvegicus Long-Evans
-
-
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
Rattus norvegicus Long-Evans
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
P07308, Q6P7B9
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
Q2KIA4, Q9TT94
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
a key step in triglyceride synthesis in the fatty acid metabolic network
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
essential enzyme activity, regulation mechanism, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, deficiency of isozyme SCD1 leads to activation of the metabolic pathways that promote fatty acid beta-oxidation in mice, enzyme regulation in the heart in a hormone-dependent fashion, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, hepatic SCD1 activity may regulate fat accumulation in the liver and possibly protects from insulin resistance in obesity, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, it is also involved in familial combined hyperlipidemia, fatty acid desaturation index, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
A7LCI9, A7LCJ0, Q64420
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, key enzyme in lipid metabolism and energy expenditure in mammals, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
Q9TT94
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
rate-limiting enzyme involved in the synthesis of monounsaturated fatty acids, which plays an important role in lipid metabolism and body weight control, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
stearoyl-CoA desaturase 2 is uniquely and absolutely required for adipogenesis, SCD2 also controls the maintenance of adipocyte-specific gene expression in fully differentiated 3T3-L1 adipocytes, including the expression of SCD1, polysome profile analysis, overview
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
stearoyl-CoA desaturase converts saturated to monounsaturated fatty acids and is a key enzyme in lipogenesis, elevated levels of endogenous lipogenesis increase the risk of fracture and suggest a role for saturated fat in the pathogenesis of osteoporosis
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
the enzyme catalyzes the desaturation from saturated to monounsaturated fatty acids
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
-
essential enzyme activity, regulation mechanism, overview
-
?
additional information
?
-
-
biosynthesis of unsaturated fatty acids. Possible substrates: acyl-CoA, acyl-acyl-carrier and acyl chains of phospholipids. The substrate in vivo is saturated phospholipid
-
-
-
additional information
?
-
-
rate limiting-step in the cellular synthesis of monounsaturated fatty acids mainly oleate and palmitoleate
-
-
-
additional information
?
-
-
key enzyme in the synthesis of unsaturated fatty acyl-CoAs
-
-
-
additional information
?
-
-
rate-limiting enzyme in the biosynthesis of monounsaturated fatty acids
-
-
-
additional information
?
-
-
incorporation of the first unsaturation bond into saturated fatty acids
-
-
-
additional information
?
-
-
long-chain polyunsaturated fatty acid biosynthetic pathway
-
-
-
additional information
?
-
-
aging human orbitofrontal cortex includes decreasing of polyunsaturated fatty acid composition associates increases in lipogenic gene expression and stearoyl-CoA desaturase activity, overview
-
-
-
additional information
?
-
-
Angus and Wagyu steers consuming high-roughage diets exhibit large differences in adipose tissue fatty acid composition, but there are no differences in terminal measures of CD activity or gene expression, overview
-
-
-
additional information
?
-
P07308, Q6P7B9
decreased degradation of SCD is responsible for the increase in palmitoyl-CoA chain elongase activity in addition to increased transcription of SCD1 in the rats treated with clofibric acid, overview
-
-
-
additional information
?
-
-
DesA3 is a membrane-bound stearoyl-CoA desaturase that works together with oxidoreductase Rv3230c, encoded by gene rv3230c, to produce oleic acid, an 55 essential constituent of mycobacterial membrane phospholipids and triglycerides
-
-
-
additional information
?
-
-
due to a population-based, longitudinal cohort study of men, the risk of fracture is highest among men with the highest levels of SCD activity index, overview
-
-
-
additional information
?
-
-
inhibition of the enzyme in cholesterol-fed hamsters leads to reduced overall body weight and adipose tissue deposition, while enzyme inhibition in absence of cholesterol does not. Enzyme inhibition induces hypercholesterinemia, overview
-
-
-
additional information
?
-
-
role of SCD1 in fatty acid metabolism in HepG2 cells, the desaturation systems in Hep-G2 cells are strongly compartmentalized, effects of SCD1 inhibition on fatty acid composition in HepG2 cells occur through changes in the dynamics of the fatty acid metabolic network and not through transcriptional regulatory mechanisms, overview
-
-
-
additional information
?
-
B7SB75, B7SB76, B7SB77, B7SB78, B7SB79
heterologous expression in yeast shows that Dpu-DELTA9-KPSE produces E9 mono-unsaturated fatty acids of various chain lengths. When provided with the (7Z)-tetradec-7-enoate, it forms the (7Z,9E)-tetradec-7,9-dienoate unsaturated fatty acids, another biosynthetic intermediate that can be chain-shortened to (5Z,7Z)-dodeca-5,7-dienoate
-
-
-
additional information
?
-
Mortierella alpina CBS 528.72
-
long-chain polyunsaturated fatty acid biosynthetic pathway
-
-
-
additional information
?
-
-
DesA3 is a membrane-bound stearoyl-CoA desaturase that works together with oxidoreductase Rv3230c, encoded by gene rv3230c, to produce oleic acid, an 55 essential constituent of mycobacterial membrane phospholipids and triglycerides
-
-
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
ascorbate
-
-
ascorbate
-
-
cytochrome b5
-
hemoprotein
-
cytochrome b5
-
-
-
cytochrome b5
-
required
-
cytochrome b5
-
dependent
-
cytochrome b5
-
-
-
cytochrome b5
-
not substituent for ferredoxin
-
cytochrome b5
-
fusion, C-terminal
-
cytochrome b5
-
no evidence for
-
cytochrome b5
-
-
-
cytochrome b5
-
-
-
cytochrome b5
-
-
-
cytochrome b5
-
-
cytochrome b5
-
-
-
FAD
-
required
ferrocytochrome b5
-
ferrocytochrome b5
-
-
ferrocytochrome b5
;
ferrocytochrome b5
;
ferrocytochrome b5
dependent on, the enzyme also requires the presence of NADH-cytochrome b5 reductase; dependent on, the enzyme also requires the presence of NADH-cytochrome b5 reductase; dependent on, the enzyme also requires the presence of NADH-cytochrome b5 reductase
flavin
-
flavin-containing NADH-cytochrome b5 reductase (EC 1.6.2.2.)
FMN
-
required, almost as active as FAD
heme
-
b-type, nonheme iron-sulfur component
heme
-
heme-containing cytochrome b5
NAD+
-
supports desaturation
NADH
-
dependent
NADH
-
preferred electron donor
NADH
-
-
NADP+
-
supports desaturation
NADPH
-
specifically required, seems not to be directly involved in the desaturation reaction but serves to keep another cofactor in the reduced state, maybe FADH
NADPH
-
absolute requirement, preferred
NADPH
-
-
NADPH
SCD is mainly dependent on NADPH, no oleic acid is produced in the absence of NADPH
heme
-
non-heme iron-containing
additional information
-
phospholipid is required
-
additional information
-
requires some other form of reduced cofactor than a reduced nicotinamide nucleotide, no special cofactor requirement
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Fe2+
-
specifically required
Fe2+
-
20-25% stimulation
Fe2+
-
iron-sulfur protein(s) may act as electron carrier(s) in place of the cytchrome b5 and NADH cytochrome b5 reductase system associated with the mammalian desaturase systems
Fe2+
-
contains one atom of non-heme iron per enzyme molecule, catalytic function
Fe2+
-
contains a non-heme iron
Fe2+
-
contains a non-heme iron
Fe2+
-
each subunit of homodimer contains one binuclear non-heme iron active site. The reduced DELTA9-desaturase has two approximately equivalent 5-coordinate irons in a distorted square pyramidal geometry, a two-in-two-out equatorial distortion, the irons are rhombic, weakly antiferromagnetically coupled. Addition of substrate causes dramatic changes, first ion remains 5-coordinate but is distorted toward a trigonal bipyramidal structure, second iron changes to 4-coordinate
Fe2+
-
heme and non-heme iron
Fe2+
-
required for activity
superoxid dismutase
-
8% stimulation
Zn2+
-
20-25% stimulation
additional information
-
no special ion requirement
additional information
-
enzyme contains active sulfhydryl groups
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1-[6-[3-(3-hydroxybenzyl)-1,2,4-oxadiazol-5-yl]pyridazin-3-yl]piperidin-4-yl)[2-(trifluoromethyl)phenyl]methanone
-
-
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-imidazol-4-yl)methanol
-
-
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)methanol
-
-
(2-[[(5-[[(4-fluoro-2-heptylphenyl)amino]methyl]thiophen-2-yl)carbonyl]amino]-1,3-thiazol-4-yl)acetic acid
-
-
(2E)-3-(4-methoxyphenyl)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]prop-2-enamide
-
-
(2R)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
(2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
-
(2S)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
(2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
-
(3-[5-[(3S)-3-(2-bromo-5-fluorophenoxy)pyrrolidin-1-yl]-1,3,4-thiadiazol-2-yl]-1,2,4-oxadiazol-5-yl)methanol
-
-
(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]phenyl)methanol
-
-
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
-
-
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
-
-
(5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]pyridin-2-yl)methanol
-
-
(5R)-5-(hydroxymethyl)-3-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridin-3-yl)-1,3-oxazolidin-2-one
-
-
(E)-N-(2-cyclopropylethyl)-N2-(pyridin-2-yl[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]methylidene)glycinamide
-
-
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
-
-
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
-
-
1'-[6-(3-methyl-1,2,4-thiadiazol-5-yl)pyridazin-3-yl]-2,3-dihydrospiro[indene-1,4'-piperidine]
-
-
1,2 diglycerides
-
only slight depression
1-(1,3-thiazol-2-yl)-4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazine
-
-
1-(1-[6-[1-(2-ethoxyethyl)-1H-pyrazol-4-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
-
-
1-(1-[6-[4-(ethoxymethyl)-1H-pyrazol-1-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
-
-
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
-
-
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)urea
-
-
1-hydroxy-3-[5-(6-[3-[2-(trifluoromethyl)benzyl]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]propan-2-one
-
-
1-[1-[6-(1-ethyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-fluoro-2,3-dihydro-1H-indole
-
-
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
-
-
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-(trifluoromethyl)-2,3-dihydro-1H-indole
-
-
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
-
-
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(5-methyl-1,3,4-thiadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(benzylcarbamoyl)-4-methyl-1,3-thiazol-2-yl]-N-(4-fluorobenzyl)-1H-1,2,3-triazole-4-carboxamide
-
-
2,3-Butanedione
-
reversible
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
2-(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)ethanol
-
-
2-(2'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-1-methyl-5-(methylsulfonyl)-2,3-dihydro-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole-6-sulfonamide
-
-
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfanyl)-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfinyl)-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-imidazo[4,5-b]pyridine
-
-
2-(2'-fluorobiphenyl-4-yl)-N,N-dimethyl-1H-benzimidazole-6-sulfonamide
-
-
2-(2'-methylbiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(2-cyclopropylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1H-isoindole-1,3(2H)-dione
-
-
2-(3'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(3'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(3'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(3'-methylbiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(4'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(4-phenoxyphenyl)-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
-
-
2-(4-phenoxyphenyl)-N-(2-phenylethyl)-1H-benzimidazole-5-carboxamide
-
-
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)-N-methylacetamide
-
-
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)ethanol
-
-
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
MF-152
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
MF-152
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxylic acid
-
-
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
-
-
2-(4-[[5-(hexylamino)-2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-N-pentylpyridine-4-carboxamide
-
-
2-(5'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(5-[1-[(2,5-dichlorophenyl)carbonyl]piperidin-4-ylidene]-2,4-dioxo-1,3-thiazolidin-3-yl)-N-pentylacetamide
-
-
2-(biphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(biphenyl-4-yl)-7-(methylsulfonyl)imidazo[1,2-a]pyridine
-
-
2-(thiophen-2-yl)-N-(2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1H-benzimidazol-5-yl)acetamide
-
-
2-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylbenzamide
-
-
2-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylbenzamide
-
-
2-acetyl-N-[1-(3,4-dichlorobenzyl)-1H-pyrazol-4-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
-
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
2-hydroxy-N-[2-[3-(1-methylethyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
CVT-12,012
2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
-
2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
-
2-mercaptoethanol
-
-
2-[(2,5-dichlorophenoxy)methyl]-N-[4-(1H-pyrazol-1-ylmethyl)phenyl]pyridine-4-carboxamide
-
-
2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]benzamide
-
-
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[1-[2-(4-fluorophenyl)ethyl]-1H-1,2,3-triazol-4-yl]-4-methyl-N-(pyridin-3-ylmethyl)-1,3-thiazole-5-carboxamide
-
-
2-[3-(4-fluorobenzyl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-N-(pyridin-3-ylmethyl)-4-(trifluoromethyl)-1,3-thiazole-5-carboxamide
-
-
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
-
-
2-[4-(2-chlorophenoxy)phenyl]-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
-
-
2-[4-(2-chlorophenoxy)phenyl]-N-(2-cyclopropylethyl)-1H-benzimidazole-5-carboxamide
-
-
2-[4-(2-chlorophenoxy)phenyl]-N-(3-methylbutyl)-1H-benzimidazole-5-carboxamide
-
-
2-[4-(2-chlorophenoxy)phenyl]-N-[(5-chlorothiophen-2-yl)methyl]-1H-benzimidazole-5-carboxamide
-
-
2-[4-(furan-3-yl)phenyl]-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-[4-(phenylcarbonyl)piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7-amine
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7-amine
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
-
-
2-[5-(2-fluorophenyl)pyridin-2-yl]-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-[6-(2-fluorophenyl)pyridin-3-yl]-6-(methylsulfonyl)-1H-benzimidazole
-
-
3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3,4-dimethoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3,4-dimethyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2,2-dihydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2,3-dihydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxy-2-methylpropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-(5-[[3-(trifluoromethyl)phenyl]carbonyl]-1,3-thiazol-2-yl)benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
-
highly potent and orally bioavailable thiazole-based SCD-1 inhibitor
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethoxy)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
potent and orally efficacious SCD-1 inhibitor
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-{5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl}benzamide
-
-
3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-[(methylsulfonyl)amino]-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
-
-
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
-
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
-
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
-
-
3-(3-hydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
-
-
3-(4-phenoxypiperidin-1-yl)-6-(5-propyl-1,2,4-oxadiazol-3-yl)pyridazine
-
-
3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
-
-
3-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazino[3,4-b][1,5]benzoxazepin-5(6H)-one
-
-
3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
-
3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
-
3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
-
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
-
-
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[3-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
-
-
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
-
-
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
-
MF-438
3-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)-N-(1,3-thiazol-2-ylmethyl)benzamide
-
-
3-([2-[4-(2,3-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2,5-dichlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-bromophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(2-hydroxyethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-2-ylmethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-3-ylmethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-4-ylmethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-ethylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbaldehyde
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbonitrile
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
-
-
3-chloro-N-[2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]pyrazin-2-amine
-
-
3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
3-methoxy-4-(2-morpholin-4-ylethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(2-phenylethyl)pyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-3-ylmethyl)pyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-4-ylmethyl)pyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-pentylpyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-propylpyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
3-[([4-[2-(acetylamino)ethyl]-2-(4-methoxyphenyl)-3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-6-yl]amino)methyl]benzoic acid
-
-
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]-N-methylpropanamide
-
-
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
3-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]propanamide
-
-
3-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]propanamide
-
-
3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid
-
-
3-[3-(2,6-dichloro-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-chloro-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
3-[3-[2-chloro-3-(trifluoromethyl)phenoxy]azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-tetrazol-5-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
-
-
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2,4-oxadiazole-5-carboxamide
-
-
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
-
-
3-[6-(4'-chlorobiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
3-[6-(4'-methylbiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
3-[6-(4-methoxyphenyl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
3-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
3-[7-oxo-6-(4-pyridin-3-ylphenyl)-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-2-ol
-
-
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-3-ol
-
-
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-4-ol
-
-
4-(1,2-benzoxazol-3-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(1H-indol-3-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
15% inhibition at 0.001 mM
4-(2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(2,3-dihydro-1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-bromo-5-fluorophenoxy)-1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3,4-thiadiazol-2-yl]piperidine
-
-
4-(2-bromophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chloro-4-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chloro-5-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chloro-6-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-phenylpiperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(1H-imidazol-2-yl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(ethylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-[(1-methylethyl)carbamoyl]phenyl]piperidine-1-carboxamide
-
-
4-(2-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-hydroxyethoxy)-3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(2-methoxyphenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(3,4-dihydroquinolin-1(2H)-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(3-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(5-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(6-hydroxy-4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
20% inhibition at 0.001 mM
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-([6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazin-3-yl]ethynyl)phenol
-
-
4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
-
-
4-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-methyl-2-[2-oxo-3-[4-(trifluoromethyl)benzyl]-2,3-dihydro-1H-imidazol-1-yl]-N-(pyridin-3-ylmethyl)-1,3-thiazole-5-carboxamide
-
-
4-[(7-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-5,6,7,7a-tetrahydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl)methoxy]benzoic acid
-
-
4-[2-(dimethylamino)ethoxy]-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]benzoic acid
-
-
5,5-dimethyl-1-pyrroline-N-oxide
-
-
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
-
5-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
5-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
5-fluoro-3-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1,2-benzoxazole
-
-
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
-
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
-
-
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
-
-
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
-
-
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
-
-
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
-
-
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
-
-
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N,N-dimethylpyridin-2-amine
-
-
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N-methylpyridine-2-carboxamide
-
-
6'-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-2,3'-bipyridine-5-carboxylic acid
-
-
6-(3,4-dihydro-1'H-spiro[chromene-2,4'-piperidin]-1'-yl)-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
-
-
6-(3-bromobenzyl)-5,7-dimethyl-N-(tetrahydrofuran-2-ylmethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxylic acid
-
-
6-(5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazol-2-yl)pyridine-3-carboxylic acid
-
-
6-(cyclopropylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
-
-
6-(ethylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-(2-phenylpyrimidin-5-yl)-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(3-methylthiophen-2-yl)phenyl]-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(pyridin-2-yl)phenyl]-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(pyridin-3-yl)phenyl]-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(pyridin-4-yl)phenyl]-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(thiophen-2-yl)phenyl]-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(thiophen-3-yl)phenyl]-1H-benzimidazole
-
-
6-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-(1-[6-[4-(trifluoromethyl)phenyl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
-
-
6-fluoro-1-(1-[6-[6-(trifluoromethyl)pyridin-3-yl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indazole
-
-
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
-
-
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(1-propyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(3-methyl-1,2,4-thiadiazol-5-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-fluorophenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methyl-1H-imidazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methylphenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(5-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(5-methylthiophen-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(6-methoxypyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(6-methylpyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-methoxy-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]naphthalene-2-carboxamide
-
-
6-methyl-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-tert-butyl-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
-
-
6-[(3,4-dichlorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
-
-
6-[(3-chloro-4-fluorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
-
-
6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine-3-carbohydrazide
-
-
6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine-3-carboxamide
-
-
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
-
-
6-[4-[(2-bromo-5-methoxyphenyl)carbonyl]piperazin-1-yl]-N-(3-phenylpropyl)pyridine-3-carboxamide
-
-
6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
-
-
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-2-amine
-
-
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
-
6-[5-chloro-2-(trifluoromethyl)benzyl]-N-hexyl-5,6,7,8-tetrahydro-1,6-naphthyridine-2-carboxamide
-
-
7-[(3-chlorobenzyl)amino]-1-(4-oxopentyl)-3-(3-pyridin-4-ylphenyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
7-[(3-chlorobenzyl)amino]-3-(4-methoxyphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
7-[(3-chlorobenzyl)amino]-3-(4-methylphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
8-(2-octylcyclopropenyl)octanoic acid
-
-
8-(trifluoromethyl)-2,5,21,24,25-pentaazatetracyclo[21.2.2.2-2,5.1-7,11]triaconta-1(25),7(28),8,10,23,26-hexaene-6,22-dione
-
-
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
-
-
A939572
-
i.e. 4-(2-chlorophenoxy)-N-(3-(3-methylcarbamoyl)phenyl)piperidine-1-carboxamide
-
adrenaline
-
-
azide
-
at high concentrations
benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
-
-
bis(salicylidene)-1,3-propanediamine
-
-
-
BVT168149
-
a property compound of Biovitrum
-
CGX0168
-
-
-
CGX0290
-
-
-
cis-10,trans-12-conjugated linoleic acid
-
-
cis-9,trans-11 conjugated linoleic acid
-
-
CN-
-
complete and reversible inhibition at 0.5 mM
CN-
-
at high concentrations
CN-
-
at high concentrations
CN-
-
44% inhibition at 1 mM
CN-
-
-
CN-
-
sensitive
CP-24879
-
9% inhibition at 0.01 mM
Cu+
-
strong, complete inhibition at 0.1 mM
Cu2+
-
and its acid chelates
Cu2+
-
and its complexes of tyrosine, histidine and lysine, act as superoxide scavengers, inhibition at low concentrations
CVT-11127
-
specific small molecule inhibitor
-
cycloheximide
-
-
cyclosporin A
-
-
cytochrome c
-
32% inhibition at 0.01 mM
cytochrome c
-
-
cytochrome c
-
very low inhibitor concentrations of 10 mM lead to an almost complete inhibition of the SCD benzamidoxime reductase activity of porcine adipose tissue microsome
decanoyl-CoA
-
competitive inhibitor
decanoyl-CoA
-
also copper complexes of tyrosine, histidine and lysine
decanoyl-CoA
-
competitive inhibition of enzyme activity greater than 95% at 0.002 mM
Dihydrolipoic acid
-
-
Dodecanoyl-CoA
-
competitive inhibitor
Dodecanoyl-CoA
-
competitive inhibition of enzyme activity greater than 90% at 0.002 mM
EDTA
-
46% inhibition at 10 mM
EDTA
-
more than 95% inhibition
ethanol
-
depression
ethyl 2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxylate
-
-
ethyl linoleate
-
-
ethyl palmitate
-
-
ethyl [5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-oxadiazol-2-yl]acetate
-
-
Fe2+
-
76% inhibition at 10 mM
glutathione
-
reduced, not marked
GSK-993
-
potent and orally available SCD1 inhibitor, almost complete inhibition at 0.01 mM
GSK-993
-
potent and orally available SCD1 inhibitor
L-cysteine
-
not marked
linoleic acid
-
-
lysophosphatidylcholine
-
-
menadione
-
85% inhibition at 0.1 mM
menadione
-
66% inhibition at 0.1 mM
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
-
-
methyl 3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxylate
-
-
methyl 8-methoxy-8-(2-octylcycloprop-1-en-1-yl)octanoate
-
methyl 9-(2-octylcycloprop-1-en-1-yl)nonanoate
-
methyl malvalate
-
methyl sterculate
inhibits the synthesis of oleic acid both with parasite lysates and infected erythrocytes, most likely by targeting SCD
methyl [5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-thiadiazol-2-yl]acetate
-
-
methylene blue
-
-
myristoyl-CoA
-
inhibitory above 0.266 mM
N,N-dimethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-(1,3-thiazol-2-yl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(1,3-thiazol-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(2-amino-2-oxoethyl)-6-(2,3-dichlorobenzyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-(2-cyclopropyl-2-hydroxyethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-4-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-3-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1H-pyrazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3,4-thiadiazole-2-carboxamide
-
-
N-(2-cyclopropylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-6-(4-[[5-fluoro-2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-6-[(1-[[2-(trifluoromethyl)phenyl]carbonyl]azetidin-3-yl)amino]pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-6-[4-[3-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxyethyl)-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
-
-
N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
-
-
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
-
-
N-(2-[2-[(3,4-dichlorobenzyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)benzamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)methanesulfonamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)propanamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)thiophene-3-carboxamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3-chloro-4-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3-chlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(4-chloro-3-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(2-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
-
N-(2-[6-[(3-chloro-4-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3-methoxybenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(4-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxopyrido[3,4-b]pyrazin-1(2H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(3,4-dimethylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(4-fluoro-3-methylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
-
N-(3-carbamoylphenyl)-4-(2-chlorophenoxy)piperidine-1-carboxamide
-
-
N-(3-methylbutyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
-
-
N-(3-methylbutyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(3-methylbutyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(3-methylbutyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(3-methylbutyl)-6-oxo-8-[[2-(trifluoromethyl)phenyl]carbonyl]-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1',2':1,6]pyrazino[2,3-c]pyridazine-3-carboxamide
-
-
N-(3-methylbutyl)-6-[[2-(trifluoromethyl)phenyl]carbonyl]-4,5,6,7-tetrahydrofuro[2,3-c]pyridine-2-carboxamide
-
-
N-(3-phenylpropyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(4-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
-
N-(5-acetyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
46% inhibition at 0.001 mM
N-(5-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
-
N-(6,7-dihydro-4H-pyrano[4,3-d][1,3]thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
-
N-(cyclopentylmethyl)-6-[5-[[2-(trifluoromethyl)phenyl]carbonyl]-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]pyridine-3-carboxamide
-
-
N-(cyclopropylmethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
-
-
N-(thiophen-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-benzyl-2-(5-hydroxy-1-oxoisoquinolin-2(1H)-yl)-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-benzyl-2-[3-(4-fluorobenzyl)-2-oxopyrrolidin-1-yl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-benzyl-2-[3-(4-fluorophenoxy)-2-oxopiperidin-1-yl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
-
-
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyridine-2-carboxamide
-
-
N-benzyl-4-(morpholin-4-ylmethyl)-2-[(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide
-
-
N-benzyl-4-methyl-2-(1-[2-[methyl(phenyl)amino]ethyl]-1H-pyrazol-3-yl)-1,3-thiazole-5-carboxamide
-
-
N-benzyl-4-methyl-2-[6-(2-phenylethyl)pyrazin-2-yl]-1,3-thiazole-5-carboxamide
-
-
N-benzyl-6-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-ethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-methoxy-3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
N-methyl-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
-
N-methyl-2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-3-carboxamide
-
-
N-methyl-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-methyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-methyl-3-[[2-oxo-2-(4-phenoxypiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
-
-
N-methyl-3-[[2-oxo-2-(4-phenylpiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
-
-
N-methyl-3-[[2-oxo-2-(4-[[2-(trifluoromethyl)phenyl]amino]piperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
-
-
N-methyl-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-imidazo[4,5-c]pyridin-4-amine
-
-
N-tert-butyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
-
-
N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-[(5-chlorothiophen-2-yl)methyl]-3-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)benzamide
-
-
N-[(6-chloropyridin-3-yl)methyl]-2-[4-[(4-fluorobenzyl)oxy]-2-oxopyridin-1(2H)-yl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-[1-[5-chloro-2-(cyclopropylmethoxy)benzyl]-5-methyl-1H-pyrazol-3-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
-
N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-[2-(4-[[2-fluoro-5-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-2-oxoethyl]-5-(2-methoxyphenyl)-1H-pyrazole-3-carboxamide
-
-
N-[2-(4-[[2-fluoro-5-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-2-oxoethyl]biphenyl-4-carboxamide
-
-
N-[2-(5-chlorothiophen-2-yl)ethyl]-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[6-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(2,2,2-trifluoroethoxy)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[4-(2,2,2-trifluoroethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-6-[(3-methylbenzyl)amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-6-[[(5-methylisoxazol-3-yl)methyl]amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-oxo-3-pyridin-3-yl-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[2-[3-(4-ethylphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-(4-methoxyphenyl)-7-[(3-methylbenzyl)amino]-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[3-tert-butyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]-2-hydroxyacetamide
-
-
N-[2-[6-(benzylamino)-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[6-[[2-fluoro-5-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[6-[[3,5-bis(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[6-[[4-fluoro-3-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
CVT-11,563
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
-
N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
-
N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(methylcarbamoyl)phenyl]-4-(2-methylphenoxy)piperidine-1-carboxamide
-
-
N-[3-(methylcarbamoyl)phenyl]-4-(2-oxo-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
7% inhibition at 0.001 mM
N-[3-(methylcarbamoyl)phenyl]-4-phenoxypiperidine-1-carboxamide
-
-
N-[3-(tert-butylcarbamoyl)phenyl]-4-(2-chlorophenoxy)piperidine-1-carboxamide
-
-
N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
N-[5-(2,5-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,4-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,4-difluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,5-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,5-difluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-chloro-4-fluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-chlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-fluoro-4-methylbenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-fluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-tert-butylbenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-methyl-1-[3-(trifluoromethyl)benzyl]-1H-pyrazol-3-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
-
N-[5-[(2-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
complete inhibition at 0.1 mM
N-[5-[(2-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
-
N-[5-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]naphthalene-2-carboxamide
-
-
N-[5-[4-fluoro-3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-{5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl}naphthalene-2-carboxamide
-
-
o-phenanthroline
-
80% inhibition at 2 mM
o-phenanthroline
-
partially inhibitory
oleoyl-CoA
-
not competitively
oleoyl-CoA
-
depression
oleyl-CoA
-
competitive, up to 50% decrease in reaction rate
p-chloromercuribenzoate
-
strong, complete inhibition at 0.02 mM
p-chloromercuribenzoate
-
a sulfonate, reversed by beta-mercaptoethanol
p-chloromercuribenzoate
-
prevention by stearoyl-CoA; reversed by beta-mercaptoethanol
p-chloromercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoate
-
potent inhibitor of the SCD benzamidoxime reductase activity of porcine adipose tissue microsomes
palmitoyl-CoA
-
depression
palmitoyl-CoA
-
competitive, up to 40% decrease in reaction rate
phenazine methosulfate
-
nearly complete inhibition at 0.3 mM
phenazine methosulfate
-
100% inhibition at 0.4 mM
Phenyllactate
-
partial inhibition, maximal at 0.08 mM
phenylpyruvate
-
partial inhibition
potassium cyanide
-
-
potassium cyanide
-
supplementation of potassium cyanide leads to a 65% inhibition of the microsomal benzamidoxime reductase activity of SCD in porcine adipose tissue
potassium hexacyanoferrate
-
-
Rapamycin
-
-
riboflavin
-
25-30% inhibition at 0.04 mM
SAR707
-
-
-
stearoyl-CoA
-
substrate inhibition above 0.05 mM
stearoyl-CoA
-
competitive, up to 50% decrease in reaction rate
stearoyl-CoA
-
inhibits SCD activity in concentrations greater than 0.05 mM
Sterculic acid
-
potent inhibitor
Sterculic acid
-
inhibits the enzyme activity in a dose dependent manner with a calculated EC50 of 247 nM
Sterculic acid
-
-
Sterculic acid
-
-
sterculic oil
-
in vivo enzyme inhibition by feeding sterculic oil
-
Tetranitromethane
-
-
Thenoyltrifluoroacetone
-
59% inhibition at 6 mM; i.e. 4,4,4-trifluoro-1-(2-thienyl)-1,3-butanedione
Thenoyltrifluoroacetone
-
i.e. 4,4,4-trifluoro-1-(2-thienyl)-1,3-butanedione
trans-10,cis-12 conjugated linoleic acid
-
inhibits stearate desaturation only, not that of palmitate
trans-10,cis-12 conjugated linoleic acid
-
95% inhibition at 0.1 mM
Trifluoperazine
-
-
[(5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-5,7a-dihydro[1,3]thiazolo[4,5-d]pyrimidin-7-yl)oxy]acetic acid
-
-
[2-(biphenyl-4-yl)-1H-benzimidazol-5-yl](phenyl)methanone
-
-
[2-([[4-([[2-(2-cyclopentylethyl)phenyl]amino]methyl)phenyl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
99% inhibition at 0.01 mM
[2-([[4-([[2-(2-cyclopentylethyl)phenyl]amino]methyl)phenyl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
-
[2-([[4-([[2-(trifluoromethyl)phenyl]amino]methyl)piperidin-1-yl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
complete inhibition at 0.01 mM
[2-([[4-([[2-(trifluoromethyl)phenyl]amino]methyl)piperidin-1-yl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
-
[2-methoxy-4-([5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]carbamoyl)phenoxy]acetic acid
-
-
[2-methoxy-5-([5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]carbamoyl)phenoxy]acetic acid
-
-
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl](phenyl)methanone
-
-
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl][2-(trifluoromethyl)phenyl]methanol
-
-
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl][2-(trifluoromethyl)phenyl]methanone
-
-
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
-
-
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
-
-
[3-(5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazol-2-yl)-1H-1,2,4-triazol-1-yl]acetic acid
-
-
[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl][2-(trifluoromethyl)phenyl]methanone
-
-
[5-(2-[3-[2-bromo-5-(trifluoromethyl)phenoxy]propoxy]-1,3-thiazol-5-yl)-2H-tetrazol-2-yl]acetic acid
-
-
[5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-oxadiazol-2-yl]methanol
-
-
[5-(5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazol-2-yl)-1H-tetrazol-1-yl]acetic acid
-
-
[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
-
-
[5-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
-
-
[5-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazin-3-yl)-1,3,4-thiadiazol-2-yl]acetic acid
-
-
[5-[2-([(2S)-3-[2-bromo-5-(trifluoromethoxy)phenoxy]-2-methylpropyl]oxy)-1,3-thiazol-5-yl]-2H-tetrazol-2-yl]acetic acid
-
-
[5-[6-(benzyloxy)pyridazin-3-yl]-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl][2-(trifluoromethyl)phenyl]methanone
-
-
[[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
-
-
additional information
-
sulfhydryl compounds
-
additional information
-
phenylalanine, indolepyruvic acid and 2-amino-1-phenylethanol show no inhibitory effect
-
additional information
-
N-ethylmaleimide and iodoacetamide have no inhibitory effect
-
additional information
-
-
-
additional information
-
not inhibitory: CoA
-
additional information
inhibition of SCD1 leads to reduction in lipid accumulation
-
additional information
-
administering CoEDTA, ytterbium acetate and chromium-mordanted straw decrease in milk cis-9 10:1/10:0, cis-9 12:1/12:0, cis-9 14:1/14:0, cis-9 16:1/16:0, cis-9 17:1/17:0, cis-9 18:1/18:0 and cis-9,trans-11 conjugated linoleic acid/trans-11 18:1 concentration rations of 44.6,52.7, 58.7, 36.8, 37.2, 44.3 and 43.0%, cows are fed with incremental levels of fish oil
-
additional information
-
design and synthesis of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone-based inhibitors, overview
-
additional information
-
design and synthesis of piperidine-aryl urea-based stearoyl-CoA desaturase1 inhibitors, overview
-
additional information
-
Co2+ has a reducing effect on the DELTA9-desaturase indices [(product of DELTA9-desaturase)/(product of DELTA9-desaturase + substrate of DELTA9-desaturase)] of milk for myristoleic acid, palmitoleic acid, oleic acid, and rumenic acid, there are no differences in DELTA9-desaturase indices between Co2+-EDTA and Co2+-acetate
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1,10-phenanthroline
-
26% stimulation
bovine serum albumin
-
stimulates activity in the microsomal fraction
-
bovine serum albumin
-
-
-
calf serum
-
-
-
catalase
-
stimulation
-
cytochrome b5 reductase
-
flavoprotein
-
cytochrome b5 reductase
-
NADH-specific, required, EC 1.6.2.2
-
cytochrome b5 reductase
-
NADH-specific, required, EC 1.6.2.2
-
cytochrome b5 reductase
-
-
-
cytochrome b5 reductase
-
NADH-dependent
-
cytochrome b5 reductase
-
-
-
Ferredoxin
-
in absence loss of desaturase activity
-
ferredoxin oxidoreductase
-
-
-
p-Cresol
-
as well as other phenols, interact with desaturase system causing a stimulation of oxidation of reduced cytochrome b5
protein
-
basic cytoplasmic protein from rat liver stimulates activity in crude extract, no activity of partially purified enzyme
protein
-
non-substrate soluble cytosolic protein stimulates
stearoyl-CoA-binding protein
-
stimulates activity in the crude microsomal fraction
-
thyroxine
-
-
triiodothyronine
-
-
Insulin
-
causes 5fold increace of activity
-
additional information
-
desaturase expression is sensitive to hormonal manipulation
-
additional information
-
high carbohydrate diet over weeks increses the stearoyl-CoA desaturase level specifically in contrast to the other lipogenic enzyme which are not upregulated, overview
-
additional information
-
SCD2 mRNA expression is elevated 44fold in adipose tissue upon feeding mice a high fat diet, whereas SCD1 shows little response
-
additional information
-
the enzyme expression is increased by feeding of cholesterol and sterculic oil in parallel, enzyme expression levels and metabolic effects, overview
-
additional information
treatment of rats with 2-(4-chlorophenoxy)-2-methylpropionic acid, i.e. clofibric acid, or feeding of a fat-free diet markedly elevated hepatic activity of SCD by increasing the steady-state level of SCD1 mRNA and enhancing transcriptional rate, metabolic effects, overview
-
additional information
-
SCD-1 activity is increased in the non-alcoholic human fatty liver, hepatic SCD-1 activity index is positively related to the concebtrations of diacylglycerols
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.001
FAD
-
-
0.003
NADH
-
-
0.089
NADH
-
-
0.038
NADPH
-
-
0.8
NADPH
-
-
0.0033
stearoyl-CoA
-
-
0.0105
stearoyl-CoA
-
in 150 mM KCl, 40 mM NaF, 100 mM sodium phosphate buffer, pH 7.4, at 37C
0.025
stearoyl-CoA
-
-
0.0566
stearoyl-CoA
in 0.1 M potassium phosphate buffer pH 7.2, at 37C
0.0025
FMN
-
-
additional information
additional information
-
substrates with 14-19 carbon fatty acyl chains show similar Km values of 0.0045-0.005 mM
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000019
N-hydroxy-benzenecarboximidamide
Sus scrofa
-
at 37C
-
0.5
stearoyl-acyl-carrier protein
Spinacia oleracea
-
-
0.35
stearoyl-CoA
Rattus norvegicus
-
25C
0.35
stearoyl-CoA
Rattus norvegicus
-
fatty acyl-CoA substrates with chain length of 14-19 carbon atoms show similar turnover number of about 22
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0001
(1-[6-[3-(3-hydroxybenzyl)-1,2,4-oxadiazol-5-yl]pyridazin-3-yl]piperidin-4-yl)[2-(trifluoromethyl)phenyl]methanone
Homo sapiens
-
IC50 below 0.0001 mM
0.000011
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-imidazol-4-yl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000017
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000002
(2E)-3-(4-methoxyphenyl)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]prop-2-enamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000003
(2E)-3-(4-methoxyphenyl)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]prop-2-enamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.008
(2R)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.03
(2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
Homo sapiens, Rattus norvegicus
-
IC50 above 0.03 mM
0.000038
(2S)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.03
(2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
Homo sapiens, Rattus norvegicus
-
IC50 above 0.03 mM
0.000022
(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]phenyl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000034
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000056
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.0000049
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.00005
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000009
(5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]pyridin-2-yl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00014
(5R)-5-(hydroxymethyl)-3-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridin-3-yl)-1,3-oxazolidin-2-one
Rattus norvegicus
-
-
0.000004
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000168
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000053
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.003
1-(1,3-thiazol-2-yl)-4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazine
Rattus norvegicus
-
-
0.000012
1-(1-[6-[1-(2-ethoxyethyl)-1H-pyrazol-4-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000008
1-(1-[6-[4-(ethoxymethyl)-1H-pyrazol-1-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000164
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000174
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00015
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)urea
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000017
1-[1-[6-(1-ethyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-fluoro-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000422
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000394
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000173
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-(trifluoromethyl)-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000268
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
Rattus norvegicus
-
-
0.001
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
Homo sapiens
-
IC50 above 0.001 mM
0.000004
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000016
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000034
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000065
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000014
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000055
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000015
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000039
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00075
1-[5-(5-methyl-1,3,4-thiadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000068
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Homo sapiens
-
-
0.0011
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.00002
2-(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)ethanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000255
2-(2'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.004489
2-(2'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.002488
2-(2'-fluorobiphenyl-4-yl)-1-methyl-5-(methylsulfonyl)-2,3-dihydro-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000074
2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole-6-sulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000343
2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole-6-sulfonamide
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000697
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfanyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000096
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfinyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000472
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfinyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000027
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000065
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000113
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-imidazo[4,5-b]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000156
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-imidazo[4,5-b]pyridine
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000528
2-(2'-fluorobiphenyl-4-yl)-N,N-dimethyl-1H-benzimidazole-6-sulfonamide
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.003863
2-(2'-methylbiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000095
2-(3'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000015
2-(3'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000148
2-(3'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000021
2-(3'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00003
2-(3'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000319
2-(3'-methylbiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000025
2-(4'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00651
2-(4-phenoxyphenyl)-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0283
2-(4-phenoxyphenyl)-N-(2-phenylethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000015
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)-N-methylacetamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000022
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)ethanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0001
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
-
0.007
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxylic acid
Rattus norvegicus
-
-
0.000004
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000024
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000278
2-(5'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00002
2-(biphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000024
2-(biphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000042
2-(biphenyl-4-yl)-7-(methylsulfonyl)imidazo[1,2-a]pyridine
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00006
2-(biphenyl-4-yl)-7-(methylsulfonyl)imidazo[1,2-a]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0032
2-(thiophen-2-yl)-N-(2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1H-benzimidazol-5-yl)acetamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00025
2-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylbenzamide
Rattus norvegicus
-
-
0.00058
2-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylbenzamide
Homo sapiens
-
-
0.0000027
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000015
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0000019
2-hydroxy-N-[2-[3-(1-methylethyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0000061
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000162
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00136
2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
Homo sapiens, Rattus norvegicus
-
-
0.00342
2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
Homo sapiens, Rattus norvegicus
-
-
0.0002
2-[(2,5-dichlorophenoxy)methyl]-N-[4-(1H-pyrazol-1-ylmethyl)phenyl]pyridine-4-carboxamide
Homo sapiens
-
-
0.000037
2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]benzamide
Homo sapiens
-
-
0.000012
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000084
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000477
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.01064
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000115
2-[4-(2-chlorophenoxy)phenyl]-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000212
2-[4-(2-chlorophenoxy)phenyl]-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000966
2-[4-(2-chlorophenoxy)phenyl]-N-(2-cyclopropylethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00272
2-[4-(2-chlorophenoxy)phenyl]-N-(3-methylbutyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000832
2-[4-(2-chlorophenoxy)phenyl]-N-[(5-chlorothiophen-2-yl)methyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000395
2-[4-(furan-3-yl)phenyl]-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.001705
2-[4-(furan-3-yl)phenyl]-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.002
2-[4-(phenylcarbonyl)piperazin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
-
0.000106
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000106
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000253
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000254
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000076
2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000153
2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000676
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.006523
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000003
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.00001
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000041
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.001019
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000097
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000378
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000038
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000319
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000257
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Homo sapiens
-
pH and temperature not specified in the publication
0.000083
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000755
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000029
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000056
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000085
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000268
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000227
2-[5-(2-fluorophenyl)pyridin-2-yl]-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000019
2-[6-(2-fluorophenyl)pyridin-3-yl]-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000058
2-[6-(2-fluorophenyl)pyridin-3-yl]-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000016
3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000022
3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000076
3,4-dimethoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000145
3,4-dimethoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.008218
3,4-dimethyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.002162
3-(2,2-dihydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00217
3-(2,2-dihydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.009999
3-(2,3-dihydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.009999 mM, in 100 mM sodium phosphate, pH 7.4, at 37C
0.009999
3-(2-hydroxy-2-methylpropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
IC50 above 0.009999 mM, in 100 mM sodium phosphate, pH 7.4, at 37C
0.0000006
3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000003
3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.001
3-(2-hydroxyethoxy)-4-methoxy-N-(5-[[3-(trifluoromethyl)phenyl]carbonyl]-1,3-thiazol-2-yl)benzamide
Mus musculus
-
IC50 above 0.001 mM, in 100 mM sodium phosphate, pH 7.4, at 37C
0.000828
3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000836
3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000002
3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
Mus musculus
-
in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37C
0.000003
3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
Homo sapiens
-
in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37C
0.000003
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethoxy)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000059
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethoxy)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000008
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00001
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000002
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000003
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000015
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000076
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000145
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.001
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.001 mM, n 100 mM sodium phosphate, pH 7.4, at 37C
0.001
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
IC50 above 0.001 mM, in 100 mM sodium phosphate, pH 7.4, at 37C
0.000006
3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000012
3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.009999
3-(2-hydroxyethoxy)-4-[(methylsulfonyl)amino]-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
IC50 above 0.009999 mM, in 100 mM sodium phosphate, pH 7.4, at 37C
0.000276
3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000884
3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00001
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Mus musculus
-
pH 7.5
0.00486
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000026
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
Mus musculus
-
pH 7.5
0.000201
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.0000074
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
Mus musculus
-
pH 7.5
0.000397
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.009999
3-(3-hydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.009999 mM, in 100 mM sodium phosphate, pH 7.4, at 37C
0.000085
3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
Mus musculus
-
pH 7.5
0.00171
3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.00133
3-(4-phenoxypiperidin-1-yl)-6-(5-propyl-1,2,4-oxadiazol-3-yl)pyridazine
Mus musculus
-
pH 7.5
0.00082
3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
Mus musculus
-
pH 7.5
0.00705
3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
Homo sapiens
-
pH 7.5
0.000035
3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.00004
3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Mus musculus
-
pH 7.5
0.000012
3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
Mus musculus
-
pH 7.5
0.000041
3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.00022
3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Mus musculus
-
pH 7.5
0.00581
3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000009
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000027
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.001992
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[3-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000023
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000023
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000021
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.0013
3-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)-N-(1,3-thiazol-2-ylmethyl)benzamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00047
3-([2-[4-(2,3-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000038
3-([2-[4-(2,5-dichlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000058
3-([2-[4-(2-bromophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000035
3-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000051
3-([2-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.0001
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(2-hydroxyethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00011
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-2-ylmethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.000099
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-3-ylmethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00011
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-4-ylmethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.000039
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-ethylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000051
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.00055
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylpyrazine-2-carboxamide
Homo sapiens
-
-
0.00021
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbaldehyde
Homo sapiens
-
-
0.00034
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbonitrile
Homo sapiens
-
-
0.000094
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00003
3-chloro-N-[2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]pyrazin-2-amine
Homo sapiens
-
-
0.0039
3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.000528
3-methoxy-4-(2-morpholin-4-ylethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.001402
3-methoxy-4-(2-morpholin-4-ylethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000193
3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000915
3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00078
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(2-phenylethyl)pyridine-2-carboxamide
Homo sapiens
-
-
0.00043
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-3-ylmethyl)pyridine-2-carboxamide
Homo sapiens
-
-
0.00035
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-4-ylmethyl)pyridine-2-carboxamide
Homo sapiens
-
-
0.01
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-pentylpyridine-2-carboxamide
Homo sapiens
-
above
0.00039
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-propylpyridine-2-carboxamide
Homo sapiens
-
-
0.00009
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.03
3-[([4-[2-(acetylamino)ethyl]-2-(4-methoxyphenyl)-3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-6-yl]amino)methyl]benzoic acid
Rattus norvegicus
-
IC50 above 0.03 mM
0.00012
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]-N-methylpropanamide
Homo sapiens
-
-
0.00036
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]-N-methylpropanamide
Rattus norvegicus
-
-
0.0000028
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Homo sapiens
-
-
0.000027
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.000177
3-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]propanamide
Homo sapiens, Rattus norvegicus
-
-
0.000513
3-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]propanamide
Homo sapiens, Rattus norvegicus
-
-
0.000266
3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.02434
3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.008167
3-[3-(2,6-dichloro-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.00004
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000067
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000019
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000028
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000021
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000023
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000163
3-[3-(2-chloro-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000072
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000022
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.03
3-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.003385
3-[3-[2-chloro-3-(trifluoromethyl)phenoxy]azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000053
3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
Mus musculus
-
pH 7.5
0.00014
3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000004
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
Mus musculus
-
below, pH 7.5
0.000014
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000017
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.0000045
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Mus musculus
-
pH 7.5
0.000026
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000037
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
-
0.000004
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
Mus musculus
-
pH 7.5
0.000208
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
Homo sapiens
-
pH 7.5
0.00001
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
Mus musculus
-
pH 7.5
0.000076
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.00037
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-tetrazol-5-yl)pyridazine
Mus musculus
-
pH 7.5
0.00002
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
Mus musculus
-
pH 7.5
0.000091
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000032
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
Mus musculus
-
pH 7.5
0.000712
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.00002
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
Mus musculus
-
pH 7.5
0.00007
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
Homo sapiens
-
pH 7.5
0.00001
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
Mus musculus
-
pH 7.5
0.000076
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000209
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000088
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
Homo sapiens
-
pH 7.5
0.000092
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
Mus musculus
-
pH 7.5
0.000004
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
Mus musculus
-
below, pH 7.5
0.000028
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
Homo sapiens
-
pH 7.5
0.001634
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2,4-oxadiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000008
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000014
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00033
3-[6-(4'-chlorobiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.0033
3-[6-(4'-chlorobiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.000134
3-[6-(4'-methylbiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.00134
3-[6-(4'-methylbiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.000145
3-[6-(4-methoxyphenyl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens, Rattus norvegicus
-
-
0.000016
3-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Homo sapiens
-
-
0.000029
3-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.00189
3-[7-oxo-6-(4-pyridin-3-ylphenyl)-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens, Rattus norvegicus
-
-
0.000336
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-2-ol
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000342
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-3-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000396
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-3-ol
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000304
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-4-ol
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.002326
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-4-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.14
4-(1,2-benzoxazol-3-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.538
4-(1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.17
4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.153
4-(2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.151
4-(2,3-dihydro-1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000004
4-(2-bromophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
below
0.00003
4-(2-bromophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000006
4-(2-chloro-4-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.000058
4-(2-chloro-4-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000004
4-(2-chloro-5-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
below
0.000018
4-(2-chloro-5-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00033
4-(2-chloro-6-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.0097
4-(2-chloro-6-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00059
4-(2-chlorophenoxy)-N-phenylpiperidine-1-carboxamide
Mus musculus
-
-
0.0075
4-(2-chlorophenoxy)-N-phenylpiperidine-1-carboxamide
Homo sapiens
-
-
0.00001
4-(2-chlorophenoxy)-N-[3-(1H-imidazol-2-yl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.00036
4-(2-chlorophenoxy)-N-[3-(1H-imidazol-2-yl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000008
4-(2-chlorophenoxy)-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.00011
4-(2-chlorophenoxy)-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000008
4-(2-chlorophenoxy)-N-[3-(ethylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.00015
4-(2-chlorophenoxy)-N-[3-(ethylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000004
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
below
0.0000078
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Rattus norvegicus
-
-
0.000037
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00081
4-(2-chlorophenoxy)-N-[3-[(1-methylethyl)carbamoyl]phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.0071
4-(2-chlorophenoxy)-N-[3-[(1-methylethyl)carbamoyl]phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000098
4-(2-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.00068
4-(2-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000003
4-(2-hydroxyethoxy)-3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00001
4-(2-hydroxyethoxy)-3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000081
4-(2-methoxyphenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.0019
4-(2-methoxyphenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.491
4-(3,4-dihydroquinolin-1(2H)-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00002
4-(3-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Mus musculus
-
-
0.00027
4-(3-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.347
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.029
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000026
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.026
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.018
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.082
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(5-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.014
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(6-hydroxy-4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.02
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.052
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.008
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.096
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.088
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.093
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000008
4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000011
4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000004
4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens, Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000007
4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000015
4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00000004
4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.0000004
4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000022
4-([6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazin-3-yl]ethynyl)phenol
Rattus norvegicus
-
-
0.000002
4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens, Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00000004
4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
Homo sapiens
-
in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37C
0.0000004
4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
Mus musculus
-
in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37C
0.000678
4-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.001218
4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.009999
4-[2-(dimethylamino)ethoxy]-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.009999 mM
0.000349
4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]benzoic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000002
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000016
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000181
5-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000165
5-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000125
5-fluoro-3-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1,2-benzoxazole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000008
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000059
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000054
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000182
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000047
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000017
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.000083
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000199
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000003
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000007
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000127
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.002823
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000017
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N,N-dimethylpyridin-2-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000035
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N-methylpyridine-2-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.001
6-(3,4-dihydro-1'H-spiro[chromene-2,4'-piperidin]-1'-yl)-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
Homo sapiens
-
IC50 below 0.001 mM
10
6-(3-bromobenzyl)-5,7-dimethyl-N-(tetrahydrofuran-2-ylmethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Rattus norvegicus
-
IC50 below 10 mM
0.0007
6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Rattus norvegicus
-
-
0.1
6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxylic acid
Rattus norvegicus
-
IC50 above 0.1 mM
0.000401
6-(cyclopropylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.001248
6-(ethylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.001308
6-(ethylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000489
6-(methylsulfonyl)-2-(2-phenylpyrimidin-5-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000472
6-(methylsulfonyl)-2-[4-(3-methylthiophen-2-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.001713
6-(methylsulfonyl)-2-[4-(pyridin-2-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00176
6-(methylsulfonyl)-2-[4-(pyridin-2-yl)phenyl]-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000425
6-(methylsulfonyl)-2-[4-(pyridin-3-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.002473
6-(methylsulfonyl)-2-[4-(pyridin-4-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.004246
6-(methylsulfonyl)-2-[4-(pyridin-4-yl)phenyl]-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000097
6-(methylsulfonyl)-2-[4-(thiophen-2-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000231
6-(methylsulfonyl)-2-[4-(thiophen-2-yl)phenyl]-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000104
6-(methylsulfonyl)-2-[4-(thiophen-3-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000035
6-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00009
6-fluoro-1-(1-[6-[4-(trifluoromethyl)phenyl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000016
6-fluoro-1-(1-[6-[6-(trifluoromethyl)pyridin-3-yl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000038
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indazole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000023
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000037
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000022
6-fluoro-1-[1-[6-(1-propyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000011
6-fluoro-1-[1-[6-(3-methyl-1,2,4-thiadiazol-5-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000777
6-fluoro-1-[1-[6-(4-fluorophenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000007
6-fluoro-1-[1-[6-(4-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000016
6-fluoro-1-[1-[6-(4-methyl-1H-imidazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000021
6-fluoro-1-[1-[6-(4-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000079
6-fluoro-1-[1-[6-(4-methylphenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000031
6-fluoro-1-[1-[6-(5-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000121
6-fluoro-1-[1-[6-(5-methylthiophen-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000012
6-fluoro-1-[1-[6-(6-methoxypyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000013
6-fluoro-1-[1-[6-(6-methylpyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000317
6-methoxy-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000005
6-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]naphthalene-2-carboxamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000009
6-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]naphthalene-2-carboxamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000286
6-methyl-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000175
6-tert-butyl-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000731
6-tert-butyl-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000015
6-[(3,4-dichlorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Homo sapiens
-
-
0.000127
6-[(3,4-dichlorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Rattus norvegicus
-
-
0.000013
6-[(3-chloro-4-fluorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Homo sapiens
-
-
0.000333
6-[(3-chloro-4-fluorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Rattus norvegicus
-
-
0.000001
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
Rattus norvegicus
-
IC50 less than 0.000039 mM, pH and temperature not specified in the publication
0.000039
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
Homo sapiens
-
IC50 less than 0.000039 mM, pH and temperature not specified in the publication
0.000074
6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
Mus musculus
-
-
0.000118
6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.00001
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000048
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Homo sapiens
-
pH and temperature not specified in the publication
0.000021
7-[(3-chlorobenzyl)amino]-1-(4-oxopentyl)-3-(3-pyridin-4-ylphenyl)pyrido[3,4-b]pyrazin-2(1H)-one
Homo sapiens
-
-
0.000157
7-[(3-chlorobenzyl)amino]-1-(4-oxopentyl)-3-(3-pyridin-4-ylphenyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
-
0.000034
7-[(3-chlorobenzyl)amino]-3-(4-methoxyphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Homo sapiens
-
-
0.00019
7-[(3-chlorobenzyl)amino]-3-(4-methoxyphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
-
0.00004
7-[(3-chlorobenzyl)amino]-3-(4-methylphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Homo sapiens
-
-
0.000343
7-[(3-chlorobenzyl)amino]-3-(4-methylphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
-
0.000039
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000162
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.03
benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens, Rattus norvegicus
-
IC50 above 0.03 mM
0.000251
benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens, Rattus norvegicus
-
-
0.00025
benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens, Rattus norvegicus
-
-
0.000865
benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens, Rattus norvegicus
-
-
0.00026
benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens, Rattus norvegicus
-
-
0.0032
benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
Homo sapiens, Rattus norvegicus
-
-
0.00172
CGX0168
Homo sapiens
-
biochemical assay
-
0.00187
CGX0168
Homo sapiens
-
cell assay
-
0.00058
CGX0290
Homo sapiens
-
cell assay
-
0.00152
CGX0290
Homo sapiens
-
biochemical assay
-
0.00088
conjugated linoleic acid
Rattus norvegicus
-
in 150 mM KCl, 40 mM NaF, 100 mM sodium phosphate buffer, pH 7.4, at 37C
-
0.000119
CVT-11,563
Homo sapiens
-
-
0.000261
CVT-11,563
Rattus norvegicus
-
-
0.0018
cytochrome c
Sus scrofa
-
at 37C
0.0383
ethyl 2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxylate
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00017
GSK-993
Homo sapiens
-
in 50 mM Tris-HCl, pH 7.4, at 25C
0.00018
GSK-993
Rattus norvegicus
-
in 50 mM Tris-HCl, pH 7.4, at 25C
0.00075
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000775
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000039
methyl 3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxylate
Homo sapiens
-
-
0.041
methyl 8-methoxy-8-(2-octylcycloprop-1-en-1-yl)octanoate
Plasmodium falciparum
Q8I0W9
in 0.1 M potassium phosphate buffer pH 7.2, at 37C
0.08
methyl 9-(2-octylcycloprop-1-en-1-yl)nonanoate
Plasmodium falciparum
Q8I0W9
in 0.1 M potassium phosphate buffer pH 7.2, at 37C
0.167
methyl malvalate
Plasmodium falciparum
Q8I0W9
in 0.1 M potassium phosphate buffer pH 7.2, at 37C
0.087
methyl sterculate
Plasmodium falciparum
Q8I0W9
in 0.1 M potassium phosphate buffer pH 7.2, at 37C
0.01
N,N-dimethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
above
0.00452
N-(1,3-thiazol-2-yl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000078
N-(1,3-thiazol-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
10
N-(2-amino-2-oxoethyl)-6-(2,3-dichlorobenzyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Rattus norvegicus
-
IC50 below 10 mM
0.0025
N-(2-cyclopropyl-2-hydroxyethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Rattus norvegicus
-
-
0.0249
N-(2-cyclopropylethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.1
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-4-carboxamide
Rattus norvegicus
-
IC50 above 0.1 mM
0.037
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
-
0.000539
N-(2-cyclopropylethyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000005
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
Mus musculus
-
-
0.00001
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000002
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
Mus musculus
-
-
0.000007
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000153
N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000292
N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000052
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000311
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000007
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000015
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000095
N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.00018
N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000028
N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000037
N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000034
N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000187
N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000007
N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000044
N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000003
N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000007
N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.00012
N-(2-hydroxyethyl)-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.00015
N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
Mus musculus
-
-
0.00082
N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
Homo sapiens
-
-
0.00025
N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
Homo sapiens
-
-
0.00037
N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
Mus musculus
-
-
0.000006
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Mus musculus
-
-
0.000006
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000009
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000099
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
Homo sapiens
-
-
0.000194
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
Mus musculus
-
-
0.00028
N-(2-[2-[(3,4-dichlorobenzyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00021
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens, Rattus norvegicus
-
-
0.00056
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)benzamide
Homo sapiens, Rattus norvegicus
-
-
0.0028
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)methanesulfonamide
Homo sapiens, Rattus norvegicus
-
-
0.0028
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)propanamide
Homo sapiens, Rattus norvegicus
-
-
0.00047
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)thiophene-3-carboxamide
Homo sapiens, Rattus norvegicus
-
-
0.00027
N-(2-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens, Rattus norvegicus
-
-
0.00075
N-(2-[2-[(3-chloro-4-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens, Rattus norvegicus
-
-
0.0013
N-(2-[2-[(3-chlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens, Rattus norvegicus
-
-
0.0009
N-(2-[2-[(4-chloro-3-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens, Rattus norvegicus
-
-
0.000549
N-(2-[6-[(2-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.000012
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Rattus norvegicus
-
-
0.000081
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00022
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00008
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Rattus norvegicus
-
-
0.0000005
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Homo sapiens
-
-
0.0000014
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Rattus norvegicus
-
-
0.000047
N-(2-[6-[(3-chloro-4-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00466
N-(2-[6-[(3-chloro-4-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0001
N-(2-[6-[(3-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.000376
N-(2-[6-[(3-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0176
N-(2-[6-[(3-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00076
N-(2-[6-[(3-methoxybenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0000078
N-(2-[6-[(4-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00011
N-(2-[6-[(4-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0000001
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxopyrido[3,4-b]pyrazin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0000086
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00011
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.000026
N-(2-[7-[(3,4-dimethylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00013
N-(2-[7-[(3,4-dimethylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0000005
N-(2-[7-[(4-fluoro-3-methylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0000031
N-(2-[7-[(4-fluoro-3-methylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00001
N-(3-carbamoylphenyl)-4-(2-chlorophenoxy)piperidine-1-carboxamide
Mus musculus
-
-
0.000059
N-(3-carbamoylphenyl)-4-(2-chlorophenoxy)piperidine-1-carboxamide
Homo sapiens
-
-
0.0216
N-(3-methylbutyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00386
N-(3-methylbutyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000434
N-(3-methylbutyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.1
N-(3-phenylpropyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.682
N-(4-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.02 - 2
N-(5-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.204
N-(6,7-dihydro-4H-pyrano[4,3-d][1,3]thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0166
N-(cyclopropylmethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000099
N-(thiophen-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00014
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00056
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyridine-2-carboxamide
Homo sapiens
-
-
0.0073
N-benzyl-6-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.00011
N-ethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.00093
N-methoxy-3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.002
N-methyl-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
-
0.001
N-methyl-2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-3-carboxamide
Homo sapiens
-
above
0.0272
N-methyl-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000097
N-methyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.0063
N-methyl-3-[[2-oxo-2-(4-phenoxypiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
Homo sapiens
-
-
0.001
N-methyl-3-[[2-oxo-2-(4-phenylpiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
Homo sapiens
-
above
0.0001
N-methyl-3-[[2-oxo-2-(4-[[2-(trifluoromethyl)phenyl]amino]piperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
Homo sapiens
-
-
0.00026
N-tert-butyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
Homo sapiens
-
-
0.000025
N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Homo sapiens, Mus musculus
-
-
0.000066
N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Mus musculus
-
-
0.000081
N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000136
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000142
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00221
N-[(5-chlorothiophen-2-yl)methyl]-3-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)benzamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000009
N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000022
N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000005
N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.000006
N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000005
N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000007
N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Mus musculus
-
-
0.00037
N-[2-(5-chlorothiophen-2-yl)ethyl]-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00018
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00033
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.01379
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[6-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00021
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(2,2,2-trifluoroethoxy)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00026
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(2,2,2-trifluoroethoxy)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000047
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000206
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00205
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[4-(2,2,2-trifluoroethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0025
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[4-(2,2,2-trifluoroethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000096
N-[2-[2-(4-methoxyphenyl)-6-[(3-methylbenzyl)amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00038
N-[2-[2-(4-methoxyphenyl)-6-[(3-methylbenzyl)amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.03
N-[2-[2-(4-methoxyphenyl)-6-[[(5-methylisoxazol-3-yl)methyl]amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
IC50 above 0.03 mM
0.000013
N-[2-[2-oxo-3-pyridin-3-yl-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000168
N-[2-[2-oxo-3-pyridin-3-yl-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000044
N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.00032
N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.0000032
N-[2-[3-(4-ethylphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000056
N-[2-[3-(4-ethylphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0000065
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000025
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0000033
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000033
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000093
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000013
N-[2-[3-(4-methoxyphenyl)-7-[(3-methylbenzyl)amino]-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000018
N-[2-[3-(4-methoxyphenyl)-7-[(3-methylbenzyl)amino]-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000261
N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00012
N-[2-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.0014
N-[2-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0028
N-[2-[3-tert-butyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00084
N-[2-[6-(benzylamino)-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00148
N-[2-[6-[[2-fluoro-5-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000051
N-[2-[6-[[3,5-bis(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000217
N-[2-[6-[[3,5-bis(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000016
N-[2-[6-[[4-fluoro-3-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00002
N-[2-[6-[[4-fluoro-3-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00000005
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.0000006
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000034
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00005
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000032
N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000049
N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
Mus musculus
-
in 100 mM sodium phosphate, pH 7.4, at 37C
0.000208
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
Homo sapiens, Rattus norvegicus
-
-
0.000261
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Homo sapiens, Rattus norvegicus
-
-
0.000268
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
Homo sapiens, Rattus norvegicus
-
-
0.0116
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
Homo sapiens, Rattus norvegicus
-
-
0.00386
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
Homo