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Assay Detail

CHEMBL641702

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Binding
Concentration required to inhibit 50% activity of Acyl coenzyme A:cholesterol acyltransferase 1 in vitro using rat liver microsome.
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
Maduskuie TP, Wilde RG, Billheimer JT, Cromley DA, Germain S, Gillies PJ, Higley CA, Johnson AL, Pennev P, Shimshick EJ.
J Med Chem (1995) 38 : 1067 -1083
PubMed 7707310 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.82 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274185 LECIMIBIDE 2.0 1 8.00
CHEMBL11612 — — 1 7.96
CHEMBL11254 — — 1 7.70
CHEMBL10954 — — 1 7.70
CHEMBL11267 — — 1 7.52
CHEMBL275332 — — 1 7.52
CHEMBL273824 — — 1 7.40
CHEMBL11445 — — 1 7.40
CHEMBL11130 — — 1 7.40
CHEMBL11201 — — 1 7.30
CHEMBL11091 — — 1 7.30
CHEMBL10844 — — 1 7.30
CHEMBL274166 — — 1 7.22
CHEMBL273532 — — 1 7.22
CHEMBL273369 — — 1 7.22
CHEMBL418529 — — 1 7.16
CHEMBL275479 — — 1 7.16
CHEMBL268478 — — 1 7.16
CHEMBL273826 — — 1 7.10
CHEMBL11422 — — 1 7.10
CHEMBL11379 — — 1 7.10
CHEMBL268699 — — 1 7.10
CHEMBL11631 — — 1 7.05
CHEMBL11303 — — 1 6.92
CHEMBL10307 — — 1 6.85
CHEMBL11232 — — 1 6.80
CHEMBL11197 — — 1 6.77
CHEMBL275308 — — 1 6.72
CHEMBL269386 — — 1 6.72
CHEMBL10916 — — 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274185 LECIMIBIDE IC50 = 10.0 nM 8.00
CHEMBL11612 — IC50 = 11.0 nM 7.96
CHEMBL10954 — IC50 = 20.0 nM 7.70
CHEMBL11254 — IC50 = 20.0 nM 7.70
CHEMBL11267 — IC50 = 30.0 nM 7.52
CHEMBL275332 — IC50 = 30.0 nM 7.52
CHEMBL11130 — IC50 = 40.0 nM 7.40
CHEMBL11445 — IC50 = 40.0 nM 7.40
CHEMBL273824 — IC50 = 40.0 nM 7.40
CHEMBL11201 — IC50 = 50.0 nM 7.30
CHEMBL11091 — IC50 = 50.0 nM 7.30
CHEMBL10844 — IC50 = 50.0 nM 7.30
CHEMBL273369 — IC50 = 60.0 nM 7.22
CHEMBL273532 — IC50 = 60.0 nM 7.22
CHEMBL274166 — IC50 = 60.0 nM 7.22
CHEMBL418529 — IC50 = 70.0 nM 7.16
CHEMBL268478 — IC50 = 70.0 nM 7.16
CHEMBL275479 — IC50 = 70.0 nM 7.16
CHEMBL273826 — IC50 = 80.0 nM 7.10
CHEMBL11422 — IC50 = 80.0 nM 7.10
CHEMBL11379 — IC50 = 80.0 nM 7.10
CHEMBL268699 — IC50 = 80.0 nM 7.10
CHEMBL11631 — IC50 = 90.0 nM 7.05
CHEMBL11303 — IC50 = 120.0 nM 6.92
CHEMBL10307 — IC50 = 140.0 nM 6.85
CHEMBL11232 — IC50 = 160.0 nM 6.80
CHEMBL11197 — IC50 = 170.0 nM 6.77
CHEMBL275308 — IC50 = 190.0 nM 6.72
CHEMBL269386 — IC50 = 190.0 nM 6.72
CHEMBL10916 — IC50 = 200.0 nM 6.70
CHEMBL269469 — IC50 = 230.0 nM 6.64
CHEMBL11400 — IC50 = 240.0 nM 6.62
CHEMBL439720 — IC50 = 260.0 nM 6.58
CHEMBL269470 — IC50 = 270.0 nM 6.57
CHEMBL11248 — IC50 = 280.0 nM 6.55
CHEMBL275265 — IC50 = 340.0 nM 6.47
CHEMBL11072 — IC50 = 350.0 nM 6.46
CHEMBL11110 — IC50 = 350.0 nM 6.46
CHEMBL416705 — IC50 = 480.0 nM 6.32
CHEMBL11316 — IC50 = 500.0 nM 6.30
CHEMBL11071 — IC50 = 640.0 nM 6.19
CHEMBL268700 — IC50 = 660.0 nM 6.18
CHEMBL273510 — IC50 = 850.0 nM 6.07
CHEMBL11204 — IC50 = 1000.0 nM 6.00
CHEMBL11526 — IC50 = 1500.0 nM 5.82
CHEMBL273825 — IC50 = 2300.0 nM 5.64
CHEMBL11192 — IC50 = 2400.0 nM 5.62
CHEMBL269463 — IC50 = 39900.0 nM 4.40
CHEMBL11238 — IC50 - nM -
CHEMBL274214 — IC50 > 50000.0 nM -