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Assay Detail

CHEMBL645898

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Binding
Inhibition against acyl coenzyme A:cholesterol acyltransferase derived from rabbit intestine microsomes
ChEMBL ↗
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acyl-CoA:cholesterol acyltransferase (CHEMBL6141) ↗
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Structure-activity relationship of a series of phenylureas linked to 4-phenylimidazole. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity. 2.
Kimura T, Watanabe N, Matsui M, Hayashi K, Tanaka H, Ohtsuka I, Saeki T, Kogushi M, Kabayashi H, Akasaka K.
J Med Chem (1993) 36 : 1641 -1653
PubMed 8496931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 75 6.76 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296094 — — 1 7.37
CHEMBL46430 — — 1 7.36
CHEMBL43422 — — 1 7.32
CHEMBL295033 — — 1 7.31
CHEMBL296463 — — 1 7.30
CHEMBL298236 — — 1 7.26
CHEMBL43989 — — 1 7.16
CHEMBL43537 — — 1 7.16
CHEMBL441429 — — 1 7.15
CHEMBL296412 — — 1 7.14
CHEMBL297770 — — 1 7.14
CHEMBL47030 — — 1 7.11
CHEMBL295867 — — 1 7.10
CHEMBL44863 — — 1 7.08
CHEMBL47095 — — 1 7.06
CHEMBL290630 — — 1 7.05
CHEMBL43908 — — 1 7.01
CHEMBL290000 — — 1 7.00
CHEMBL46756 — — 1 7.00
CHEMBL296714 — — 1 6.92
CHEMBL43592 — — 1 6.89
CHEMBL46450 — — 1 6.89
CHEMBL295184 — — 1 6.85
CHEMBL295171 — — 1 6.85
CHEMBL297454 — — 1 6.85
CHEMBL417896 — — 1 6.85
CHEMBL295616 — — 1 6.82
CHEMBL42760 — — 1 6.82
CHEMBL46861 — — 1 6.80
CHEMBL295878 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296094 — IC50 = 43.0 nM 7.37
CHEMBL46430 — IC50 = 44.0 nM 7.36
CHEMBL43422 — IC50 = 48.0 nM 7.32
CHEMBL295033 — IC50 = 49.0 nM 7.31
CHEMBL296463 — IC50 = 50.0 nM 7.30
CHEMBL298236 — IC50 = 55.0 nM 7.26
CHEMBL43989 — IC50 = 69.0 nM 7.16
CHEMBL43537 — IC50 = 70.0 nM 7.16
CHEMBL441429 — IC50 = 71.0 nM 7.15
CHEMBL296412 — IC50 = 73.0 nM 7.14
CHEMBL297770 — IC50 = 73.0 nM 7.14
CHEMBL47030 — IC50 = 77.0 nM 7.11
CHEMBL295867 — IC50 = 80.0 nM 7.10
CHEMBL44863 — IC50 = 84.0 nM 7.08
CHEMBL47095 — IC50 = 88.0 nM 7.06
CHEMBL290630 — IC50 = 90.0 nM 7.05
CHEMBL43908 — IC50 = 97.0 nM 7.01
CHEMBL290000 — IC50 = 100.0 nM 7.00
CHEMBL46756 — IC50 = 100.0 nM 7.00
CHEMBL296714 — IC50 = 120.0 nM 6.92
CHEMBL43592 — IC50 = 130.0 nM 6.89
CHEMBL46450 — IC50 = 130.0 nM 6.89
CHEMBL417896 — IC50 = 140.0 nM 6.85
CHEMBL297454 — IC50 = 140.0 nM 6.85
CHEMBL295184 — IC50 = 140.0 nM 6.85
CHEMBL295171 — IC50 = 140.0 nM 6.85
CHEMBL295616 — IC50 = 150.0 nM 6.82
CHEMBL42760 — IC50 = 150.0 nM 6.82
CHEMBL46861 — IC50 = 160.0 nM 6.80
CHEMBL295878 — IC50 = 160.0 nM 6.80
CHEMBL43675 — IC50 = 160.0 nM 6.80
CHEMBL44318 — IC50 = 170.0 nM 6.77
CHEMBL42165 — IC50 = 170.0 nM 6.77
CHEMBL46769 — IC50 = 180.0 nM 6.75
CHEMBL42477 — IC50 = 180.0 nM 6.75
CHEMBL277986 CL-277082 IC50 = 180.0 nM 6.75
CHEMBL295466 — IC50 = 190.0 nM 6.72
CHEMBL44848 — IC50 = 200.0 nM 6.70
CHEMBL45033 — IC50 = 210.0 nM 6.68
CHEMBL288332 — IC50 = 210.0 nM 6.68
CHEMBL44755 — IC50 = 210.0 nM 6.68
CHEMBL47093 — IC50 = 220.0 nM 6.66
CHEMBL43603 — IC50 = 220.0 nM 6.66
CHEMBL297553 — IC50 = 230.0 nM 6.64
CHEMBL297185 — IC50 = 230.0 nM 6.64
CHEMBL43107 — IC50 = 230.0 nM 6.64
CHEMBL294932 — IC50 = 230.0 nM 6.64
CHEMBL47084 — IC50 = 250.0 nM 6.60
CHEMBL42821 — IC50 = 260.0 nM 6.58
CHEMBL42296 — IC50 = 280.0 nM 6.55