Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL646540

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro inhibition of rat intestinal acyl coenzyme A:cholesterol acyltransferase using [1-14C]oleolyl-CoA
ChEMBL ↗
89
Total Activities
82
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

Sterol O-acyltransferase 1 (CHEMBL285) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo.
O'Brien PM, Sliskovic DR, Blankley CJ, Roth BD, Wilson MW, Hamelehle KL, Krause BR, Stanfield RL.
J Med Chem (1994) 37 : 1810 -1822
PubMed 8021920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 89 6.59 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296055 — — 1 7.77
CHEMBL53249 — — 3 7.48
CHEMBL54304 — — 3 7.41
CHEMBL53989 — — 1 7.35
CHEMBL298666 — — 1 7.35
CHEMBL52365 — — 1 7.35
CHEMBL300462 — — 1 7.35
CHEMBL52857 — — 1 7.32
CHEMBL444579 — — 2 7.32
CHEMBL54724 — — 1 7.31
CHEMBL55001 — — 1 7.30
CHEMBL432118 — — 1 7.29
CHEMBL52233 — — 1 7.29
CHEMBL52617 — — 1 7.28
CHEMBL298941 — — 2 7.22
CHEMBL53797 — — 1 7.19
CHEMBL22373 CL-976 — 1 7.14
CHEMBL53994 — — 1 7.11
CHEMBL53597 — — 1 7.10
CHEMBL301119 — — 1 7.10
CHEMBL54809 — — 1 7.10
CHEMBL54129 — — 1 7.09
CHEMBL300915 — — 1 7.08
CHEMBL51666 — — 1 7.05
CHEMBL52189 — — 1 6.96
CHEMBL53227 — — 1 6.96
CHEMBL296163 — — 1 6.96
CHEMBL52517 — — 1 6.92
CHEMBL50261 — — 1 6.92
CHEMBL299331 — — 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296055 — IC50 = 17.0 nM 7.77
CHEMBL53249 — IC50 = 33.0 nM 7.48
CHEMBL54304 — IC50 = 39.0 nM 7.41
CHEMBL53989 — IC50 = 45.0 nM 7.35
CHEMBL298666 — IC50 = 45.0 nM 7.35
CHEMBL52365 — IC50 = 45.0 nM 7.35
CHEMBL300462 — IC50 = 45.0 nM 7.35
CHEMBL444579 — IC50 = 48.0 nM 7.32
CHEMBL52857 — IC50 = 48.0 nM 7.32
CHEMBL54304 — IC50 = 48.0 nM 7.32
CHEMBL54724 — IC50 = 49.0 nM 7.31
CHEMBL55001 — IC50 = 50.0 nM 7.30
CHEMBL432118 — IC50 = 51.0 nM 7.29
CHEMBL52233 — IC50 = 51.0 nM 7.29
CHEMBL53249 — IC50 = 51.0 nM 7.29
CHEMBL53249 — IC50 = 53.0 nM 7.28
CHEMBL52617 — IC50 = 52.0 nM 7.28
CHEMBL298941 — IC50 = 60.0 nM 7.22
CHEMBL53797 — IC50 = 64.0 nM 7.19
CHEMBL54304 — IC50 = 70.0 nM 7.16
CHEMBL22373 CL-976 IC50 = 73.0 nM 7.14
CHEMBL53994 — IC50 = 77.0 nM 7.11
CHEMBL53597 — IC50 = 79.0 nM 7.10
CHEMBL54809 — IC50 = 80.0 nM 7.10
CHEMBL301119 — IC50 = 80.0 nM 7.10
CHEMBL54129 — IC50 = 81.0 nM 7.09
CHEMBL300915 — IC50 = 83.0 nM 7.08
CHEMBL51666 — IC50 = 90.0 nM 7.05
CHEMBL444579 — IC50 = 99.0 nM 7.00
CHEMBL296163 — IC50 = 110.0 nM 6.96
CHEMBL53227 — IC50 = 110.0 nM 6.96
CHEMBL52189 — IC50 = 110.0 nM 6.96
CHEMBL52517 — IC50 = 120.0 nM 6.92
CHEMBL50261 — IC50 = 120.0 nM 6.92
CHEMBL299331 — IC50 = 130.0 nM 6.89
CHEMBL300297 — IC50 = 140.0 nM 6.85
CHEMBL53857 — IC50 = 150.0 nM 6.82
CHEMBL298941 — IC50 = 150.0 nM 6.82
CHEMBL300081 — IC50 = 150.0 nM 6.82
CHEMBL52973 — IC50 = 150.0 nM 6.82
CHEMBL299188 — IC50 = 160.0 nM 6.80
CHEMBL53922 — IC50 = 170.0 nM 6.77
CHEMBL416665 — IC50 = 200.0 nM 6.70
CHEMBL300617 — IC50 = 230.0 nM 6.64
CHEMBL52185 — IC50 = 250.0 nM 6.60
CHEMBL54549 — IC50 = 270.0 nM 6.57
CHEMBL298682 — IC50 = 300.0 nM 6.52
CHEMBL50351 — IC50 = 330.0 nM 6.48
CHEMBL296153 — IC50 = 350.0 nM 6.46
CHEMBL54180 — IC50 = 370.0 nM 6.43