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Assay Detail

CHEMBL814213

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Binding
In vitro inhibitory activity against Squalene Synthase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Squalene synthase (CHEMBL3815)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

(1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent squalene synthase inhibitor.
Fung AK, Baker WR, Fakhoury S, Stein HH, Cohen J, Donner BG, Garvey DS, Spina KP, Rosenberg SH.
J Med Chem (1997) 40 : 2123 -2125
PubMed 9216829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.28 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303461 1 7.89
CHEMBL304119 1 7.85
CHEMBL445618 1 7.43
CHEMBL303235 1 6.89
CHEMBL68289 1 6.85
CHEMBL306441 1 6.75
CHEMBL304850 1 6.14
CHEMBL302702 1 5.85
CHEMBL68005 1 5.85
CHEMBL67051 1 5.10
CHEMBL67614 1 5.10
CHEMBL305004 1 5.00
CHEMBL302010 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303461 IC50 = 13.0 nM 7.89
CHEMBL304119 IC50 = 14.0 nM 7.85
CHEMBL445618 IC50 = 37.0 nM 7.43
CHEMBL303235 IC50 = 130.0 nM 6.89
CHEMBL68289 IC50 = 140.0 nM 6.85
CHEMBL306441 IC50 = 180.0 nM 6.75
CHEMBL304850 IC50 = 720.0 nM 6.14
CHEMBL302702 IC50 = 1400.0 nM 5.85
CHEMBL68005 IC50 = 1400.0 nM 5.85
CHEMBL67051 IC50 = 8000.0 nM 5.10
CHEMBL67614 IC50 = 8000.0 nM 5.10
CHEMBL305004 IC50 = 10000.0 nM 5.00
CHEMBL302010 IC50 = 10000.0 nM 5.00