Literature summary for 5.4.99.7 extracted from

Brown, G.R.; Hollinshead, D.M.; Stokes, E.S.; Clarke, D.S.; Eakin, M.A.; Foubister, A.J.; Glossop, S.C.; Griffiths, D.; Johnson, M.C.; McTaggart, F.; Mirrlees, D.J.; Smith, G.J.; Wood, R.
Quinuclidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase: optimization from lipid profiles (1999), J. Med. Chem., 42, 1306-1311.

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Inhibitors

Inhibitors	Comment	Organism	Structure
(Z)-3-[4-(4-bromobenzoyl)phenacylidene]quinuclidine	IC50: 83 nM, oral and selective inhibition of cholesterol biosynthesis derived from enzyme inhibition	Homo sapiens
(Z)-3-[4-(4-bromobenzoyl)phenacylidene]quinuclidine	IC50: 124 nM, oral and selective inhibition of cholesterol biosynthesis derived from enzyme inhibition	Rattus norvegicus
3-[(4-chlorobenzoyl)-4-phenoxy]quinuclidin-3-ol	-	Homo sapiens
3-[(4-chlorobenzoyl)-4-phenoxy]quinuclidin-3-ol	-	Rattus norvegicus
3-[(4-chlorobenzoyl)-4-phenoxy]quinuclidine	-	Homo sapiens
3-[(4-chlorobenzoyl)-4-phenoxy]quinuclidine	-	Rattus norvegicus
3-[2-(4-bromobenzophenone)ethynyl]quinuclidin-3-ol	-	Homo sapiens
3-[2-(4-bromobenzophenone)ethynyl]quinuclidin-3-ol	-	Rattus norvegicus

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
microsome	-	Rattus norvegicus	-	-

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Rattus norvegicus	-	-	-

Synonyms

Synonyms	Comment	Organism
2,3-oxidosqualene cyclase-lanosterol synthase	-	Homo sapiens
2,3-oxidosqualene cyclase-lanosterol synthase	-	Rattus norvegicus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000083	-	IC50: 83 nM, oral and selective inhibition of cholesterol biosynthesis derived from enzyme inhibition	Homo sapiens	(Z)-3-[4-(4-bromobenzoyl)phenacylidene]quinuclidine
0.000124	-	IC50: 124 nM, oral and selective inhibition of cholesterol biosynthesis derived from enzyme inhibition	Rattus norvegicus	(Z)-3-[4-(4-bromobenzoyl)phenacylidene]quinuclidine

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Release 2023.1 (January 2023)