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Literature summary for 5.4.99.7 extracted from

  • Fouchet, M.H.; Donche, F.; Martin, C.; Bouillot, A.; Junot, C.; Boullay, A.B.; Potvain, F.; Magny, S.D.; Coste, H.; Walker, M.; Issandou, M.; Dodic, N.
    Design and evaluation of a novel series of 2,3-oxidosqualene cyclase inhibitors with low systemic exposure, relationship between pharmacokinetic properties and ocular toxicity (2008), Bioorg. Med. Chem., 16, 6218-6232.
    View publication on PubMed
Search for more literature for 5.4.99.7

Inhibitors

Inhibitors Comment Organism Structure
1-[4-(trifluoromethoxy)phenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmeth yl]-piperazine
-
 Homo sapiens
1-[4-chlorobenzyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-chlorophenylcarbonyl]-4-[4-(1-methyl-pyrazol-4-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
1-[4-chlorophenylcarbonyl]-4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
1-[4-chlorophenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-chlorophenylcarbonyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-1-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-3-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
1-[4-chlorophenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-chlorophenylsulfonyl]-4-[3-(pyridin-4-yl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-chlorophenylsulfonyl]-4-[4-(4-methylpiperazin-1-yl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-chlorophenylsulfonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-chlorophenylsulfonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-methoxyphenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
 Homo sapiens
1-[4-trifluoroacetyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
BIBB 515
-
 Homo sapiens
N-[2-(4-(3-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide inactive at 200 nM Homo sapiens
N-[2-(4-(4-((pyrrolidin-1-yl)methyl)phenyl)phenyl)ethyl]-4-chlorobenzenesulfonamide
-
 Homo sapiens
N-[2-(4-(4-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
-
 Homo sapiens
Ro48-8071
-
 Homo sapiens
U18666A
-
 Homo sapiens
ZD-9720
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(S)-2,3-oxidosqualene
-
 Homo sapiens lanosterol
-
 ?
2,3:22,23-diepoxysqualene
-
 Homo sapiens 24(S),25-epoxylanosterol
-
 ?

Synonyms

Synonyms Comment Organism
2,3-Oxidosqualene cyclase
-
 Homo sapiens
2,3-oxidosqualene:lanosterol cyclase
-
 Homo sapiens
OSC
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
-
 Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
0.00000585
-
-
 Homo sapiens BIBB 515
0.000006
-
-
 Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[4-(4-methylpiperazin-1-yl)phenylmethyl]-piperazine
0.000013
-
-
 Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
0.00002
-
-
 Homo sapiens 1-[4-(trifluoromethoxy)phenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmeth yl]-piperazine
0.000028
-
-
 Homo sapiens N-[2-(4-(4-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
0.000032
-
-
 Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
0.000032
-
-
 Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
0.00004
-
-
 Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
0.000063
-
-
 Homo sapiens N-[2-(4-(4-((pyrrolidin-1-yl)methyl)phenyl)phenyl)ethyl]-4-chlorobenzenesulfonamide
0.0002
-
-
 Homo sapiens N-[2-(4-(3-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
0.0002
-
-
 Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-1-yl)phenylmethyl]-piperazine
0.0002
-
-
 Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-3-yl)phenylmethyl]-piperazine
0.0002
-
-
 Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(1-methyl-pyrazol-4-yl)phenylmethyl]-piperazine
0.0002
-
-
 Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenylmethyl]-piperazine
0.0002
-
-
 Homo sapiens 1-[4-trifluoroacetyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
0.000316
-
-
 Homo sapiens 1-[4-chlorobenzyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
0.0005
-
-
 Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[3-(pyridin-4-yl)phenylmethyl]-piperazine
0.002511
-
-
 Homo sapiens 1-[4-methoxyphenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine