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Assay Detail

CHEMBL646536

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

Binding
Acyl coenzyme A:cholesterol acyltransferase (ACAT), inhibition by incubation with [1-14C]oleolyl-CoA and intestinal microsomes isolated from intestinal mucosa of cholesterol-fed rabbits
ChEMBL ↗
72
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Intestinal mucosa
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond.
Roark WH, Roth BD, Holmes A, Trivedi BK, Kieft KA, Essenburg AD, Krause BR, Stanfield RL.
J Med Chem (1993) 36 : 1662 -1668
PubMed 8496932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 72 6.47 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42603 — — 1 7.75
CHEMBL47218 — — 1 7.68
CHEMBL297985 — — 1 7.55
CHEMBL44652 — — 1 7.43
CHEMBL46510 — — 1 7.37
CHEMBL46689 — — 1 7.37
CHEMBL40519 — — 1 7.36
CHEMBL295248 — — 1 7.35
CHEMBL43257 — — 1 7.34
CHEMBL417531 — — 1 7.34
CHEMBL46481 — — 1 7.33
CHEMBL47640 — — 1 7.32
CHEMBL46480 — — 1 7.30
CHEMBL42897 — — 1 7.28
CHEMBL41330 — — 1 7.28
CHEMBL42673 — — 1 7.25
CHEMBL297135 — — 1 7.16
CHEMBL44760 — — 1 7.14
CHEMBL47105 — — 1 7.06
CHEMBL45093 — — 1 7.00
CHEMBL42343 — — 1 7.00
CHEMBL44480 — — 1 6.96
CHEMBL42354 — — 1 6.80
CHEMBL46690 — — 1 6.75
CHEMBL42602 — — 1 6.70
CHEMBL46586 — — 1 6.68
CHEMBL44334 — — 1 6.60
CHEMBL46417 — — 1 6.50
CHEMBL47221 — — 1 6.47
CHEMBL46376 — — 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42603 — IC50 = 18.0 nM 7.75
CHEMBL47218 — IC50 = 21.0 nM 7.68
CHEMBL297985 — IC50 = 28.0 nM 7.55
CHEMBL44652 — IC50 = 37.0 nM 7.43
CHEMBL46510 — IC50 = 43.0 nM 7.37
CHEMBL46689 — IC50 = 43.0 nM 7.37
CHEMBL40519 — IC50 = 44.0 nM 7.36
CHEMBL295248 — IC50 = 45.0 nM 7.35
CHEMBL43257 — IC50 = 46.0 nM 7.34
CHEMBL417531 — IC50 = 46.0 nM 7.34
CHEMBL46481 — IC50 = 47.0 nM 7.33
CHEMBL47640 — IC50 = 48.0 nM 7.32
CHEMBL46480 — IC50 = 50.0 nM 7.30
CHEMBL42897 — IC50 = 52.0 nM 7.28
CHEMBL41330 — IC50 = 52.0 nM 7.28
CHEMBL42673 — IC50 = 56.0 nM 7.25
CHEMBL297135 — IC50 = 70.0 nM 7.16
CHEMBL44760 — IC50 = 73.0 nM 7.14
CHEMBL47105 — IC50 = 87.0 nM 7.06
CHEMBL45093 — IC50 = 99.0 nM 7.00
CHEMBL42343 — IC50 = 100.0 nM 7.00
CHEMBL44480 — IC50 = 110.0 nM 6.96
CHEMBL42354 — IC50 = 160.0 nM 6.80
CHEMBL46690 — IC50 = 180.0 nM 6.75
CHEMBL42602 — IC50 = 200.0 nM 6.70
CHEMBL46586 — IC50 = 210.0 nM 6.68
CHEMBL44334 — IC50 = 250.0 nM 6.60
CHEMBL46417 — IC50 = 320.0 nM 6.50
CHEMBL47221 — IC50 = 340.0 nM 6.47
CHEMBL46376 — IC50 = 400.0 nM 6.40
CHEMBL45379 — IC50 = 500.0 nM 6.30
CHEMBL45429 — IC50 = 520.0 nM 6.28
CHEMBL298465 — IC50 = 610.0 nM 6.21
CHEMBL298465 — IC50 = 610.0 nM 6.21
CHEMBL444831 — IC50 = 630.0 nM 6.20
CHEMBL46744 — IC50 = 690.0 nM 6.16
CHEMBL44331 — IC50 = 860.0 nM 6.07
CHEMBL416626 — IC50 = 900.0 nM 6.05
CHEMBL46985 — IC50 = 900.0 nM 6.05
CHEMBL47206 — IC50 = 980.0 nM 6.01
CHEMBL47522 — IC50 = 1100.0 nM 5.96
CHEMBL44885 — IC50 = 1200.0 nM 5.92
CHEMBL42902 — IC50 = 2460.0 nM 5.61
CHEMBL295580 — IC50 = 2900.0 nM 5.54
CHEMBL415924 — IC50 = 3100.0 nM 5.51
CHEMBL297184 — IC50 = 3300.0 nM 5.48
CHEMBL46966 — IC50 = 4500.0 nM 5.35
CHEMBL297460 — IC50 = 4700.0 nM 5.33
CHEMBL46460 — IC50 = 5400.0 nM 5.27
CHEMBL44423 — IC50 = 5400.0 nM 5.27