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Assay Detail

CHEMBL4418324

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Binding
Inhibition of ACAT2 in mouse hepatic microsome membranes using [1-14C]oleoyl coenzyme A as substrate incubated for 5 mins
ChEMBL ↗
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sterol O-acyltransferase 2 (CHEMBL2653) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Pyripyropene derivatives having acat2 inhibiting activity and stable to metabolizing enzymes
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 9.20 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2375704 — — 1 9.30
CHEMBL3936419 — — 1 9.30
CHEMBL2375700 — — 1 9.30
CHEMBL2398812 — — 1 9.30
CHEMBL3898848 — — 1 9.30
CHEMBL2398805 — — 1 9.30
CHEMBL2375692 — — 1 9.30
CHEMBL2398808 — — 1 9.30
CHEMBL2398813 — — 1 9.30
CHEMBL2375707 — — 1 9.30
CHEMBL3899506 — — 1 9.30
CHEMBL3981954 — — 1 9.30
CHEMBL3943599 — — 1 9.30
CHEMBL3974636 — — 1 9.30
CHEMBL2398810 — — 1 9.30
CHEMBL2375703 — — 1 9.30
CHEMBL2398811 — — 1 9.30
CHEMBL3954976 — — 1 9.30
CHEMBL3958342 — — 1 9.30
CHEMBL2375706 — — 1 9.30
CHEMBL2398807 — — 1 9.00
CHEMBL2398804 — — 1 9.00
CHEMBL2375604 — — 1 9.00
CHEMBL3913788 — — 1 9.00
CHEMBL2334205 — — 1 9.00
CHEMBL4518651 — — 1 9.00
CHEMBL3901614 — — 1 9.00
CHEMBL2375698 — — 1 9.00
CHEMBL2375702 — — 1 9.00
CHEMBL2398814 — — 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2375704 — IC50 = 0.5 nM 9.30
CHEMBL3936419 — IC50 = 0.5 nM 9.30
CHEMBL2375700 — IC50 = 0.5 nM 9.30
CHEMBL2398812 — IC50 = 0.5 nM 9.30
CHEMBL3898848 — IC50 = 0.5 nM 9.30
CHEMBL2398805 — IC50 = 0.5 nM 9.30
CHEMBL2375692 — IC50 = 0.5 nM 9.30
CHEMBL2398808 — IC50 = 0.5 nM 9.30
CHEMBL2398813 — IC50 = 0.5 nM 9.30
CHEMBL2375707 — IC50 = 0.5 nM 9.30
CHEMBL3899506 — IC50 = 0.5 nM 9.30
CHEMBL3981954 — IC50 = 0.5 nM 9.30
CHEMBL3943599 — IC50 = 0.5 nM 9.30
CHEMBL3974636 — IC50 = 0.5 nM 9.30
CHEMBL2398810 — IC50 = 0.5 nM 9.30
CHEMBL2375703 — IC50 = 0.5 nM 9.30
CHEMBL2398811 — IC50 = 0.5 nM 9.30
CHEMBL3954976 — IC50 = 0.5 nM 9.30
CHEMBL3958342 — IC50 = 0.5 nM 9.30
CHEMBL2375706 — IC50 = 0.5 nM 9.30
CHEMBL2375698 — IC50 = 1.0 nM 9.00
CHEMBL2398807 — IC50 = 1.0 nM 9.00
CHEMBL2398804 — IC50 = 1.0 nM 9.00
CHEMBL2375604 — IC50 = 1.0 nM 9.00
CHEMBL3913788 — IC50 = 1.0 nM 9.00
CHEMBL2334205 — IC50 = 1.0 nM 9.00
CHEMBL4518651 — IC50 = 1.0 nM 9.00
CHEMBL3901614 — IC50 = 1.0 nM 9.00
CHEMBL2375702 — IC50 = 1.0 nM 9.00
CHEMBL2398814 — IC50 = 1.0 nM 9.00
CHEMBL3899035 — IC50 < 0.5 nM -
CHEMBL2398809 — IC50 < 0.5 nM -
CHEMBL2398806 — IC50 < 0.5 nM -
CHEMBL2375602 — IC50 < 0.5 nM -
CHEMBL2375699 — IC50 < 0.5 nM -