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Literature summary 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

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.4.99.7 1-[4-(trifluoromethoxy)phenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmeth yl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorobenzyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorophenylcarbonyl]-4-[4-(1-methyl-pyrazol-4-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
5.4.99.7 1-[4-chlorophenylcarbonyl]-4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
5.4.99.7 1-[4-chlorophenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorophenylcarbonyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-1-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
5.4.99.7 1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-3-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
5.4.99.7 1-[4-chlorophenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorophenylsulfonyl]-4-[3-(pyridin-4-yl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorophenylsulfonyl]-4-[4-(4-methylpiperazin-1-yl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorophenylsulfonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-chlorophenylsulfonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-methoxyphenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
-
Homo sapiens
5.4.99.7 1-[4-trifluoroacetyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine inactive at 200 nM Homo sapiens
5.4.99.7 BIBB 515
-
Homo sapiens
5.4.99.7 N-[2-(4-(3-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide inactive at 200 nM Homo sapiens
5.4.99.7 N-[2-(4-(4-((pyrrolidin-1-yl)methyl)phenyl)phenyl)ethyl]-4-chlorobenzenesulfonamide
-
Homo sapiens
5.4.99.7 N-[2-(4-(4-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
-
Homo sapiens
5.4.99.7 Ro48-8071
-
Homo sapiens
5.4.99.7 U18666A
-
Homo sapiens
5.4.99.7 ZD-9720
-
Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
5.4.99.7 microsome
-
Homo sapiens
-
-

Organism

EC Number Organism UniProt Comment Textmining
5.4.99.7 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.4.99.7 Hep-G2 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.4.99.7 (S)-2,3-oxidosqualene
-
Homo sapiens lanosterol
-
?
5.4.99.7 2,3:22,23-diepoxysqualene
-
Homo sapiens 24(S),25-epoxylanosterol
-
?

Synonyms

EC Number Synonyms Comment Organism
5.4.99.7 2,3-Oxidosqualene cyclase
-
Homo sapiens
5.4.99.7 2,3-oxidosqualene:lanosterol cyclase
-
Homo sapiens
5.4.99.7 OSC
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.4.99.7 0.000003
-
-
Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
5.4.99.7 0.00000585
-
-
Homo sapiens BIBB 515
5.4.99.7 0.000006
-
-
Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[4-(4-methylpiperazin-1-yl)phenylmethyl]-piperazine
5.4.99.7 0.000013
-
-
Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
5.4.99.7 0.00002
-
-
Homo sapiens 1-[4-(trifluoromethoxy)phenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmeth yl]-piperazine
5.4.99.7 0.000028
-
-
Homo sapiens N-[2-(4-(4-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
5.4.99.7 0.000032
-
-
Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
5.4.99.7 0.000032
-
-
Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
5.4.99.7 0.00004
-
-
Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(dimethylaminomethyl)phenylmethyl]-piperazine
5.4.99.7 0.000063
-
-
Homo sapiens N-[2-(4-(4-((pyrrolidin-1-yl)methyl)phenyl)phenyl)ethyl]-4-chlorobenzenesulfonamide
5.4.99.7 0.0002
-
-
Homo sapiens N-[2-(4-(3-dimethylaminomethylphenyl)phenyl)ethyl]-4-cyanobenzenesulfonamide
5.4.99.7 0.0002
-
-
Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-1-yl)phenylmethyl]-piperazine
5.4.99.7 0.0002
-
-
Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(pyrazol-3-yl)phenylmethyl]-piperazine
5.4.99.7 0.0002
-
-
Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(1-methyl-pyrazol-4-yl)phenylmethyl]-piperazine
5.4.99.7 0.0002
-
-
Homo sapiens 1-[4-chlorophenylcarbonyl]-4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenylmethyl]-piperazine
5.4.99.7 0.0002
-
-
Homo sapiens 1-[4-trifluoroacetyl]-4-[4-(imidazol-1-yl)phenylmethyl]-piperazine
5.4.99.7 0.000316
-
-
Homo sapiens 1-[4-chlorobenzyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine
5.4.99.7 0.0005
-
-
Homo sapiens 1-[4-chlorophenylsulfonyl]-4-[3-(pyridin-4-yl)phenylmethyl]-piperazine
5.4.99.7 0.002511
-
-
Homo sapiens 1-[4-methoxyphenylcarbonyl]-4-[4-(pyridin-4-yl)phenylmethyl]-piperazine