Information on EC 2.7.11.26 - tau-protein kinase and Organism(s) Homo sapiens

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Homo sapiens


The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.26
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RECOMMENDED NAME
GeneOntology No.
tau-protein kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + [tau-protein] = ADP + O-phospho-[tau-protein]
show the reaction diagram
activation loop structure, substrate binding structure, and catalytic site structure and mechanism
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
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-
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SYSTEMATIC NAME
IUBMB Comments
ATP:[tau-protein] O-phosphotransferase
Activated by tubulin. Involved in the formation of paired helical filaments, which are the main fibrous component of all fibrillary lesions in brain and are associated with Alzheimer's disease.
CAS REGISTRY NUMBER
COMMENTARY hide
111694-09-8
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
show the reaction diagram
-
-
-
-
?
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
show the reaction diagram
-
-
-
-
?
ATP + cAMP response element-binding protein
ADP + phosphorylated cAMP response element-binding protein
show the reaction diagram
-
-
-
-
?
ATP + CEP164
ADP + phospho-CEP164
show the reaction diagram
-
-
-
?
ATP + CEP97
ADP + phospho-CEP97
show the reaction diagram
-
-
-
?
ATP + coronavirus nucleocapsid protein
ADP + phosphorylated coronavirus nucleocapsid protein
show the reaction diagram
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phosphorylation sites are at Ser177, Ser181, Ser184, Ser185, Ser187, Ser189, Ser191, Ser203, and Ser207
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-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
show the reaction diagram
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-
-
-
?
ATP + cyclin D1
ADP + phosphorylated cyclin D1
show the reaction diagram
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
show the reaction diagram
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-
-
-
?
ATP + DIWKKFELLPTPPLSPSRRSG
ADP + DIWKKFELLP(P)TPPL(P)SPSRRSG
show the reaction diagram
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c-Myc
-
?
ATP + DIWKKFELVPSPPTSPPWGL
ADP + DIWKKFELVP(P)SPPT(P)SPPWGL
show the reaction diagram
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L-myc
-
?
ATP + EEPQTVPEMPGETPPLSPIDMESQER
ADP + EEPQTVPEMPGE(P)TPPL(P)SPIDMESQER
show the reaction diagram
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c-Jun
-
?
ATP + eIF2B peptide
ADP + phosphorylated eIF2B peptide
show the reaction diagram
-
-
-
-
?
ATP + FITC-GSRSRTPSLP
ADP + FITC-GSRSRTP-phosphoserine-LP
show the reaction diagram
-
synthetic fluorescence-labeled peptide substrate derived from residues 207-216 of tau protein, phosphorylation of S214 by SGK1
-
-
?
ATP + FXVEXTPXCFSRXSSLSSLS
ADP + ?
show the reaction diagram
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-
-
-
?
ATP + glycogen synthase
ADP + glycogen synthase phosphate
show the reaction diagram
-
-
-
-
?
ATP + heat shock factor-1
ADP + phosphorylated heat shock factor-1
show the reaction diagram
-
-
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
show the reaction diagram
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isoenzyme TPKII
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-
?
ATP + JHMV-N protein
ADP + phosphorylated JHMV-N protein
show the reaction diagram
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phosphorylation sites are at Ser197, Ser201, Ser-205, and Ser-209
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-
?
ATP + Jun
ADP + phosphorylated Jun
show the reaction diagram
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-
-
-
?
ATP + KRREILSRRPpSYR
ADP + ?
show the reaction diagram
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KRREILSRRPpSYR is selectively phosphorylated by GSK-3 and therefore acts as a competitive inhibitor of other GSK-3 substrates
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?
ATP + LLNASGSTSTPAPSRTASFSESR
ADP + LLNASGSTS(P)TPAP(P)SRTASFSESR
show the reaction diagram
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ATP-citrate lyase
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?
ATP + MAP2
ADP + MAP2 phosphate
show the reaction diagram
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isoenzyme TPKII
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-
?
ATP + Myc
ADP + phosphorylated Myc
show the reaction diagram
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-
-
-
?
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + p53 phosphate
show the reaction diagram
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-
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
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-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
ATP + pyruvate dehydrogenase
ADP + pyruvate dehydrogenase phosphate
show the reaction diagram
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PDH is phosphorylated and inactivated in vitro and also in betaA-treated hippocampal cultures, resulting in mitochondrial dysfunction which will contribute to neuronal death
-
-
?
ATP + RSRSRSRSRSRSPPPVSK
ADP + phosphorylated RSRSRSRSRSRSPPPVSK
show the reaction diagram
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SC35-derived peptide 180-197, recombinant GSK-3beta
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-
?
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
ATP + SPPLSPIDMETQER
ADP + (P)SPPLSPIDME(P)TQER
show the reaction diagram
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JunD
-
?
ATP + SPVVSGDT(P)SPR
ADP + ?
show the reaction diagram
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-
-
-
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ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
ATP + TDP-43
ADP + phospho-TDP-43
show the reaction diagram
-
-
-
?
ATP + TPPKSPSAAK
ADP + TPPK(P)SPSAAK
show the reaction diagram
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protein tau
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?
ATP + tubulin
ADP + phospho-tubulin
show the reaction diagram
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-
-
?
ATP + [amyloid precursor protein]
ADP + O-phospho-[amyloid precursor protein]
show the reaction diagram
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phosphorylation of the intracellular domain Thr668 of APP by GSK-3beta
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?
ATP + [FRAT-2 protein]
ADP + phosphorylated [FRAT-2 protein]
show the reaction diagram
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i.e. frequently rearranged in advanced T-cell lymphoma protein 2, phosphorylation by GSK3beta
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-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
show the reaction diagram
protein tau + ATP
phosphorylated protein tau + ADP
show the reaction diagram
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the microtubule-associated protein tau is the principal component of the paired helical filaments - PHFs - found in the brains of patients with Alzheimer disease, and PHF-tau is hyperphosphorylated
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?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
show the reaction diagram
-
-
-
-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
show the reaction diagram
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase
ADP + glycogen synthase phosphate
show the reaction diagram
-
-
-
-
?
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
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substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors
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-
?
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
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tau in Alzheimer disease brain is highly phosphorylated and aggregates into paired helical filaments comprising characteristic neurofibrillary tangles, overview
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?
ATP + tubulin
ADP + phospho-tubulin
show the reaction diagram
Q6IQ55
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-
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?
ATP + [amyloid precursor protein]
ADP + O-phospho-[amyloid precursor protein]
show the reaction diagram
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phosphorylation of the intracellular domain Thr668 of APP by GSK-3beta
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?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Zn2+
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high zinc concentrations (0.1-0.5 mM) increase glycogen synthase kinase-3beta phosphorylation on tyrosine 216, a phosphorylation associated with increased activity of this tau kinase, whereas the phosphorylation of GSK-3alpha at Y279 and the level of total GSK-3beta are not affected
additional information
-
not activated by K+, Ca2+ or Zn2+
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2'Z,3'E)-6-bromoindirubin-3'-oxime
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(4-amino-2-((4-chlorophenyl)amino)thiazol-5-yl)(3-nitrophenyl)methanone
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enzyme binding structure analysis
1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
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1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
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1-(cyclopropylmethyl)-3-[4-(5,6-difluoro-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indole-5-carbonitrile
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1-ethyl-3-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)urea
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1-methyl-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
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1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
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2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
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2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
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2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
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2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
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2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
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2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
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2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole
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2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
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2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
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-
2-(3-ethylpiperazin-1-yl)-N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]acetamide
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2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
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2-amino-N-(2'-(cyclohex-2''-enyl)acetyl)acetimide
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2-amino-N-(2'-(phenyl)acetyl)propanimide
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2-chloro-5-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
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2-chloro-5-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
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2-chloro-5-[[4-(2-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
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2-chloro-5-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
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-
2-chloro-5-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
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2-chloro-5-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
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2-chloro-5-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
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2-methyl-N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
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2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
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2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
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2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
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2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
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2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
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-
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
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-
3-(1-(2-(1H-imidazol-1-yl)ethyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
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3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
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3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-1-phenyl-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
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-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
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-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
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3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
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3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
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3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(4-(1H-imidazol-1-yl)butyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(1-methyl-7-phenoxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
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-
3-(1-benzofuran-3-yl)-4-(5-cyclopropyl-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-hydroxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-iodo-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(7-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[1-(3-hydroxypropyl)-5-phenoxy-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[1-methyl-5-(morpholin-4-yl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[5-(benzyloxy)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[5-bromo-1-(3-hydroxypropyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[7-(methoxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(2-morpholinoethyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(2-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(2-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(3-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(3-nitrophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[methyl(phenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(4-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(4-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(5,6-difluoro-1-benzofuran-3-yl)-4-(1-methyl-1H-benzo[g]indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5,7-dibromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(4-methoxyphenoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-en-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-yn-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-chloro-1-methyl-1H-indol-3-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-hydroxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(methoxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-6-iodo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-methoxy-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-methoxy-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5H-[1,3]dioxolo[4,5-f]indol-7-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-bromo-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclobutylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclopropylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(6-fluoro-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-fluoro-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(7-methoxy-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(7-methoxy-1-benzofuran-3-yl)-4-[1-methyl-6-(trifluoromethyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(imidazo[1,2-a]pyridin-3-yl)-4-[2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl]-1H-pyrrole-2,5-dione
-
an imidazo[1,2-a]pyridinylindolylmaleimide
3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
-
-
3-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
-
-
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(4-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[(4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(5E)-5-methyl-4-oxo-2-hydroxy-5-octenyl]glutarimide
-
-
3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
-
3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
-
3-[1H-indol-3-yl]-4-[2-[4-methylpiperazin-1-yl]quinazolin-4-yl]-1H-pyrrole-2,5-dione
-
enzyme binding structure analysis
3-[4-(6-ethyl-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1-methyl-1H-indole-5-carbonitrile
-
-
3-[5-(cyclopropylethynyl)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-[6-(4-chlorophenyl)-5-fluoro-1-methyl-1H-indol-3-yl]-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-[6-(hydroxymethyl)-1-benzofuran-3-yl]-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-[methyl(phenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[methyl(phenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(4-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
-
-
4-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
4-[1-cyclohexyl-4-[4-fluorophenyl]-1H-imidazol-5-yl]pyrimidin-2-amine
-
enzyme binding structure analysis
4-{(2R)-2-[(1R,3R,5S)-3,5-dimethyl-2-oxocyclohexyl]-2-hydroxyethyl}piperidine-2,6-dione
-
-
5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
-
-
5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
-
-
5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
-
-
5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-amine
-
-
5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-amine
-
-
5-phenyl[1,2]oxazolo[5,4-b]pyridin-3-amine
-
-
5-[2-phenylpyrazolo[1,5-a]pyridin-3-yl]-1h-pyrazolo[3,4-c]pyridazin-3-amine
-
enzyme binding structure analysis
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
-
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
-
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
-
-
6-O-methyl-7-O-alpha-L-rhamnopyranosyldaidzein
-
-
7-methoxy-1-methyl-9h-betacarboline
-
enzyme binding structure analysis
7-O-alpha-L-rhamnopyranosyldaidzein
-
-
AMP-PNP
-
ATP analogue adenosine 5'-(beta,gamma-imino)triphosphate
CT99021
inhibition of GSK3 with CT99021 has little effect on the relative level of phosphorylation of Ser199 or Ser404 of human tau, but inhibition of GSK3beta using CT99021 results in dephosphorylation of endogenous c-Jun, Inh-2 and beta-catenin and dramatically increased c-Myc and beta-catenin expression
cycloheximide
-
-
disheveled protein
-
-
-
DMSO
-
complete inhibition at 0.4% (v/v)
enzastaurin
-
activation-related phosphorylation of Y216/Y276 is dramatically decreased following exposure to enzastaurin whereas the inhibitory phosphorylation of S21 is significantly up-regulated in glioma cells. GSK3 inhibition results in glioma cell death and reduced tumorigenicity
GF 109203X
GSK-3 inhibitor IX
-
-
kenpaullone
-
-
KRM-189
-
74% inhibition at 0.01 mM, competes with ATP for GSK-3beta, leading to decreased Vmax and constant Km with increasing concentrations of ATP
KRM-191
-
84% inhibition at 0.01 mM, competes with ATP for GSK-3beta, leading to decreased Vmax and constant Km with increasing concentrations of ATP
KRM-192
-
75% inhibition at 0.01 mM
KRM-195
-
80% inhibition at 0.01 mM
KRM-296
-
65% inhibition at 0.01 mM
KRM-7777
-
65% inhibition at 0.01 mM
leptin
-
-
-
lithium
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
-
-
N-(1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
N-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)butanamide
-
-
N-(5,6-diphenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)-4-methylpiperidine-1-carboxamide
-
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-chloro-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-cyano-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-phenyl-1H-indazol-3-yl)butanamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopentanecarboxamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)methanesulfonamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-yl)butanamide
-
-
N-(5-phenyl-1H-pyrazolo[4,3-d]pyrimidin-3-yl)butanamide
-
-
N-(6-phenyl-1H-indazol-3-yl)cyclopropanecarboxamide
-
-
N-(6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-[3-cyano-6-[3-[1-piperidinyl]propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]1-naphthalenecarboxamide
-
enzyme binding structure analysis
N-[4-[3-(4-ethylpiperazin-1-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[3-(dimethylamino)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[3-(morpholin-4-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[ethyl(piperidin-1-ylmethyl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[methyl(piperidin-1-yl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(2-chlorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(2-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(3-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(6,6-difluorocyclohexa-1,3-dien-1-yl)-4-[3-(dimethylamino)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[5-(biphenyl-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(naphthalen-1-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(naphthalen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-(4-ethylpiperazin-1-yl)butanamide
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-bromo-6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-2-(4-methylpiperidin-1-yl)acetamide
-
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-chloro-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-phenyl-4-[3-(pyrrolidin-1-yl)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[6-(1H-indol-5-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2,5-difluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2H-pyrrol-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-bromo-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-chloro-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-fluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-sulfamoylphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-5-methyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(furan-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(thiophen-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(thiophen-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
naramycin B
-
-
Ro 31-8220
roscovitine
-
complete inhibition of T231 phosphorylation by 25-Cdk5 kinase complex
SB-216763
-
specific inhibitor of GSK-3beta
SB-415286
SB415286
-
-
SRN-003-556
-
-
staurosporine
trans-activating transcriptor-eIF2B
-
acts as a competitive inhibitor of GSK-3
-
ZM336372
-
inhibits GSK-3beta through phosphorylation at Ser9, a dose-dependent increase in phosphorylation of GSK-3beta occurs after treatment with ZM336372 (0.025-0.1 mM)
[3R]-1-[5-methyl-7Hpyrrolo[2,3-d]pyrimidin-4-yl]pyrrolidin-3-amine
-
enzyme binding structure analysis
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
14-3-3
-
protein 14-3-3 recognises GSK-3 phosphorylated at Ser9, and the association of tau with this complex is believed to regulate its phosphorylation by GSK-3, since in human embryonic kidney cells, tau phosphorylation by GSK-3 is suppressed in the absence of 14-3-3, but GSK-3 is active and phosphorylates tau if 14-3-3 is present
-
AMP
-
AMP binding induces a conformational change in the ? -subunit activation loop of the kinase that allows phosphorylation of the activating residue Thr172 by AMPK upstream kinases
AT7519
-
0.0005 mM AT7519 inhibits glycogen synthase kinase 3beta phosphorylation, AT7519 dephosphorylates GSK-3beta independent of inhibition of transcription
cAMP
-
required for PKA activation
forskolin
-
forskolin specifically induces tau hyperphosphorylation by PKA at Ser214 resulting in increased phosphorylation at Ser199, Ser22, Ser396, and Ser404 in N2a/tau441 cells, forskolin has no effect on GSK-3
FRAT-2
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, activates phosphorylation of primed sites of tau protein about 8fold, no effect on unprimed site phosphorylation
-
heparansulfate
-
heparin is more effective than heparan sulfate at lower concentrations in inducing the hyperphosphorylation of tau by GSK3beta
heparin
L-Dopa
-
activates GSK-3beta at high dose
p25
-
inducible cytotoxic expression factor required for Cdk5 activity, formation of a complex with Cdk5, p25 overexpression increases tau phosphorylation rate
-
protein 14-3-3
-
protein 14-3-3 facilitates tau phosphorylation by SGK1 and regulates its subcellular localization
-
soluble beta-amyloid oligomers
-
activate GSK-3beta mediated tau phosphorylation and increase toxicity, reduced content of soluble, not insoluble, amyloid oligomers reduces the tau phosphorylation activity, specific antibodies can inhibit the activation, overview
-
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.002
(4-amino-2-((4-chlorophenyl)amino)thiazol-5-yl)(3-nitrophenyl)methanone
Homo sapiens
-
pH and temperature not specified in the publication
0.0000025
1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000086
1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000125 - 0.000131
1-(cyclopropylmethyl)-3-[4-(5,6-difluoro-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indole-5-carbonitrile
0.00281
1-ethyl-3-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)urea
Homo sapiens
-
-
0.023
1-methyl-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
Homo sapiens
-
-
0.0000094
1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000065
2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000049
2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000044
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000054
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00022
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00034
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00068
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000068
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000057
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000021
2-(3-ethylpiperazin-1-yl)-N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]acetamide
Homo sapiens
-
-
0.00021
2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000143
2-chloro-5-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
Homo sapiens
-
-
0.000074
2-chloro-5-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000028
2-chloro-5-[[4-(2-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000076
2-chloro-5-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000085
2-chloro-5-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000026
2-chloro-5-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000109
2-chloro-5-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000019
2-methyl-N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
Homo sapiens
-
-
0.000094
2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000013
2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0002
2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00028
2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000084
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000025
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00026
3-(1-(2-(1H-imidazol-1-yl)ethyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00645
3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.07334
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-1-phenyl-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00066
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00021
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.00055
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.01358
3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00129
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.01245
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00114
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00015
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0116
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.00179
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00085
3-(1-(4-(1H-imidazol-1-yl)butyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00053
3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
3-(1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00022
3-(1-benzofuran-3-yl)-4-(1-methyl-7-phenoxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000007
3-(1-benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000235
3-(1-benzofuran-3-yl)-4-(5-cyclopropyl-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000026
3-(1-benzofuran-3-yl)-4-(5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00036
3-(1-benzofuran-3-yl)-4-(5-fluoro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00069
3-(1-benzofuran-3-yl)-4-(5-hydroxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000345
3-(1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000184
3-(1-benzofuran-3-yl)-4-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00044
3-(1-benzofuran-3-yl)-4-(6-chloro-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000015
3-(1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000223
3-(1-benzofuran-3-yl)-4-(6-iodo-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000055
3-(1-benzofuran-3-yl)-4-(7-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00022
3-(1-benzofuran-3-yl)-4-[1-(3-hydroxypropyl)-5-phenoxy-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.001304
3-(1-benzofuran-3-yl)-4-[1-methyl-5-(morpholin-4-yl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00165
3-(1-benzofuran-3-yl)-4-[5-(benzyloxy)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000016
3-(1-benzofuran-3-yl)-4-[5-bromo-1-(3-hydroxypropyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0009
3-(1-benzofuran-3-yl)-4-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000054
3-(1-benzofuran-3-yl)-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00000012
3-(1-benzofuran-3-yl)-4-[7-(methoxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00026
3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0009
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(2-morpholinoethyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00076
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00204
3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.00192
3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0306
3-(1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000187
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000131
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000161
3-(2,3-dihydro-1H-indol-1-yl)-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000694
3-(2,3-dihydro-1H-indol-1-yl)-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000337
3-(2-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000216
3-(2-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000093
3-(2-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000195
3-(2-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000374
3-(2-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000161
3-(2-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000216
3-(2-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00011
3-(2-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00046
3-(3-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000058
3-(3-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.001478
3-(3-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000532
3-(3-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000203
3-(3-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000141
3-(3-nitrophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.001412
3-(4-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000514
3-(4-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000091
3-(4-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000447
3-(4-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000407
3-(4-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000317
3-(4-chlorophenyl)-4-[(4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.002285
3-(4-chlorophenyl)-4-[methyl(phenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000529
3-(4-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00039
3-(4-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000243
3-(4-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000314
3-(5,6-difluoro-1-benzofuran-3-yl)-4-(1-methyl-1H-benzo[g]indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000887
3-(5,7-dibromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00014
3-(5-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00055
3-(5-bromo-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000075
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000335
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(4-methoxyphenoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00000051
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000483
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-en-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000253
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-yn-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000042
3-(5-chloro-1-methyl-1H-indol-3-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00067
3-(5-fluoro-1-benzofuran-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00018
3-(5-fluoro-1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000014
3-(5-fluoro-1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000035
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-hydroxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00000035
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000238
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(methoxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000247
3-(5-fluoro-6-iodo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00048
3-(5-methoxy-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.02246
3-(5-methoxy-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00057
3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.000708
3-(5H-[1,3]dioxolo[4,5-f]indol-7-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00095
3-(6-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00226
3-(6-bromo-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00101
3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.00036
3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.000866
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000114
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.004092
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclobutylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00104
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclopropylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00000095
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00031
3-(6-fluoro-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.01244
3-(6-fluoro-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00016
3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.00018
3-(7-methoxy-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000831
3-(7-methoxy-1-benzofuran-3-yl)-4-[1-methyl-6-(trifluoromethyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.01186
3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.000091
3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000014
3-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
Homo sapiens
-
-
0.00424
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.00059
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000291
3-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
Homo sapiens
-
-
0.000082
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000052
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000142
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00002
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000083
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000071
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000149
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000152
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-chlorophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000139
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000104
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000094
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-chlorophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000059
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000173
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(4-chlorophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000114
3-[(3-chlorophenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000104
3-[(3-chlorophenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000257
3-[(3-chlorophenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00007
3-[(3-chlorophenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000156
3-[(3-chlorophenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000301
3-[(3-chlorophenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000259
3-[(3-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000251
3-[(3-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000472
3-[(3-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000236
3-[(3-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000481
3-[(3-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000704
3-[(3-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000123
3-[(4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000023
3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000035
3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000021
3-[1H-indol-3-yl]-4-[2-[4-methylpiperazin-1-yl]quinazolin-4-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0000132
3-[4-(6-ethyl-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1-methyl-1H-indole-5-carbonitrile
Homo sapiens
-
-
0.0000226
3-[5-(cyclopropylethynyl)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.007
3-[6-(4-chlorophenyl)-5-fluoro-1-methyl-1H-indol-3-yl]-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00016
3-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0000051
3-[6-(hydroxymethyl)-1-benzofuran-3-yl]-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.001398
3-[methyl(phenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.002613
3-[methyl(phenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000136
3-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000134
3-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000195
3-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000079
3-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000186
3-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000214
3-[[4-(4-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000152
3-[[4-(methylsulfanyl)phenyl]amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000392
3-[[4-(methylsulfanyl)phenyl]amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000404
3-[[4-(methylsulfanyl)phenyl]amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00025
4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
Homo sapiens
-
-
0.023
4-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
Homo sapiens
-
-
0.00013
4-[1-cyclohexyl-4-[4-fluorophenyl]-1H-imidazol-5-yl]pyrimidin-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00033
5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000016
5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000028
5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00043
5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
Homo sapiens
-
-
0.00053
5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
Homo sapiens
-
-
0.00126
5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-amine
Homo sapiens
-
-
0.023
5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-amine
Homo sapiens
-
-
0.023
5-phenyl[1,2]oxazolo[5,4-b]pyridin-3-amine
Homo sapiens
-
-
0.0019
5-[2-phenylpyrazolo[1,5-a]pyridin-3-yl]-1h-pyrazolo[3,4-c]pyridazin-3-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000031
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000065
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000018
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00035
7-methoxy-1-methyl-9h-betacarboline
Homo sapiens
-
pH and temperature not specified in the publication
0.000548
KRM-189
Homo sapiens
-
-
0.000467
KRM-191
Homo sapiens
-
-
0.001012
KRM-192
Homo sapiens
-
-
0.001863
KRM-195
Homo sapiens
-
-
0.000539
KRM-296
Homo sapiens
-
-
0.007149
KRM-7777
Homo sapiens
-
-
0.000071
LiCl
Homo sapiens
-
-
0.00063
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
Homo sapiens
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.002343
N-(1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
Homo sapiens
-
-
0.000691
N-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)butanamide
Homo sapiens
-
-
0.000415
N-(5,6-diphenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000383
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)-4-methylpiperidine-1-carboxamide
Homo sapiens
-
-
0.000075
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000234
N-(5-chloro-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000087
N-(5-cyano-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000099
N-(5-phenyl-1H-indazol-3-yl)butanamide
Homo sapiens
-
-
0.000291
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide
Homo sapiens
-
-
0.000056
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
Homo sapiens
-
-
0.000005
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopentanecarboxamide
Homo sapiens
-
-
0.003572
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)methanesulfonamide
Homo sapiens
-
-
0.000043
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
Homo sapiens
-
-
0.000007
N-(5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-yl)butanamide
Homo sapiens
-
-
0.002697
N-(5-phenyl-1H-pyrazolo[4,3-d]pyrimidin-3-yl)butanamide
Homo sapiens
-
-
0.000498
N-(6-phenyl-1H-indazol-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000425
N-(6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.0032
N-[3-cyano-6-[3-[1-piperidinyl]propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]1-naphthalenecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
N-[4-[3-(4-ethylpiperazin-1-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000022
N-[4-[3-(dimethylamino)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000005
N-[4-[3-(morpholin-4-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000005
N-[4-[ethyl(piperidin-1-ylmethyl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000009
N-[4-[methyl(piperidin-1-yl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000007
N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000027
N-[5-(2-chlorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000018
N-[5-(2-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.00002
N-[5-(3-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000356
N-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000005
N-[5-(6,6-difluorocyclohexa-1,3-dien-1-yl)-4-[3-(dimethylamino)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000851
N-[5-(biphenyl-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000241
N-[5-(naphthalen-1-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000169
N-[5-(naphthalen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000011
N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000443
N-[5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000004
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-(4-ethylpiperazin-1-yl)butanamide
Homo sapiens
-
-
0.000001
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
Homo sapiens
-
-
0.0000008
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000007
N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000016
N-[5-bromo-6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000018
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-2-(4-methylpiperidin-1-yl)acetamide
Homo sapiens
-
-
0.000007
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000001
N-[5-chloro-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000011
N-[5-phenyl-4-[3-(pyrrolidin-1-yl)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000042
N-[6-(1H-indol-5-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.001
N-[6-(2,5-difluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000036
N-[6-(2-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.001593
N-[6-(2-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.00032
N-[6-(2H-pyrrol-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000008
N-[6-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000005
N-[6-(3-bromo-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000007
N-[6-(3-chloro-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000828
N-[6-(3-fluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000012
N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000125
N-[6-(3-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000481
N-[6-(3-sulfamoylphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000015
N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000012
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
Homo sapiens
-
-
0.000008
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000006
N-[6-(4-hydroxyphenyl)-5-methyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000024
N-[6-(4-hydroxyphenyl)-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.023
N-[6-(4-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000141
N-[6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000035
N-[6-(furan-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000099
N-[6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000215
N-[6-(thiophen-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000039
N-[6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000329
N-[6-(thiophen-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000028 - 0.0002
staurosporine
0.0032
[3R]-1-[5-methyl-7Hpyrrolo[2,3-d]pyrimidin-4-yl]pyrrolidin-3-amine
Homo sapiens
-
pH and temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.26
-
in the presence of Mg2+
0.57
-
in the presence of Mn2+
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
HeLa cells
Manually annotated by BRENDA team
-
purified recombinant GSK-3beta
Manually annotated by BRENDA team
-
U251, T98, U87, U373, U118, A172
Manually annotated by BRENDA team
-
weak expression
Manually annotated by BRENDA team
-
weak expression
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
mainly
Manually annotated by BRENDA team
additional information
TTBK2 localization sites include the centriole/basal body, the midbody, and possibly the mitotic spindles. Localization at the base of primary cilia
-
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
23000
-
1 * 30000 + 1 * 23000, catalytic and regulatory subunit, SDS-PAGE
35000
-
gel filtration
38620
-
calculated
39000
-
1 * 39000, SDS-PAGE
47000
-
SDS-PAGE
72000
-
SDS-PAGE
100000
-
immunoprecipitation, lysosomal degradation product of full-length TTBK1
142700
-
predicted
230000
-
immunoprecipitation, full-length TTBK1 migrates to 230 kDa because of the negative charge of the polyglutamate sequence and the protein modification