Assay Detail
Binding
CHEMBL4265762
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ACAT in arterial homogenates isolated from 1% cholesterol fed New Zealand White rabbit assessed as reduction in cholesteryl oleate formation incubated for 5 mins in presence of [14C]-oleoyl-CoA and BSA complex by TLC method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of Clinical Candidate 2-(4-(2-((1 H-Benzo[ d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)- N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.34 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4247249 | — | — | 1 | 8.40 |
| CHEMBL4294841 | — | — | 1 | 7.92 |
| CHEMBL4280317 | — | — | 1 | 7.80 |
| CHEMBL4287597 | — | — | 1 | 7.72 |
| CHEMBL4277672 | — | — | 1 | 7.62 |
| CHEMBL4279691 | — | — | 1 | 7.60 |
| CHEMBL4288312 | — | — | 1 | 7.58 |
| CHEMBL4282905 | — | — | 1 | 7.48 |
| CHEMBL4283167 | — | — | 1 | 7.47 |
| CHEMBL4294713 | — | — | 1 | 7.44 |
| CHEMBL4242494 | — | — | 1 | 7.44 |
| CHEMBL4281138 | — | — | 1 | 7.39 |
| CHEMBL4286811 | — | — | 1 | 7.30 |
| CHEMBL4288347 | — | — | 1 | 7.08 |
| CHEMBL4242551 | — | — | 1 | 7.02 |
| CHEMBL4284218 | — | — | 1 | 6.96 |
| CHEMBL4294421 | — | — | 1 | 6.96 |
| CHEMBL4291768 | — | — | 1 | 6.92 |
| CHEMBL4293342 | — | — | 1 | 6.89 |
| CHEMBL4291024 | — | — | 1 | 6.64 |
| CHEMBL4294442 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4247249 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4294841 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4280317 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4287597 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4277672 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4279691 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4288312 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4282905 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4283167 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4294713 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4242494 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4281138 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4286811 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4288347 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4242551 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4284218 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4294421 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4291768 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4293342 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4291024 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4294442 | — | IC50 | = | 300.0 | nM | 6.52 |