Assay Detail
Binding
CHEMBL4265763
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ACAT in New Zealand White rabbit intestinal microsomes assessed as reduction in cholesteryl oleate formation incubated for 3 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 |
| Tissue | Intestine |
| Subcellular | Microsomes |
| 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 | 6.90 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4247249 | — | — | 1 | 7.68 |
| CHEMBL4282905 | — | — | 1 | 7.54 |
| CHEMBL4280317 | — | — | 1 | 7.44 |
| CHEMBL4294841 | — | — | 1 | 7.43 |
| CHEMBL4281138 | — | — | 1 | 7.42 |
| CHEMBL4287597 | — | — | 1 | 7.41 |
| CHEMBL4286811 | — | — | 1 | 7.29 |
| CHEMBL4279691 | — | — | 1 | 7.19 |
| CHEMBL4242494 | — | — | 1 | 7.11 |
| CHEMBL4277672 | — | — | 1 | 7.03 |
| CHEMBL4242551 | — | — | 1 | 6.89 |
| CHEMBL4294713 | — | — | 1 | 6.75 |
| CHEMBL4291768 | — | — | 1 | 6.68 |
| CHEMBL4288312 | — | — | 1 | 6.60 |
| CHEMBL4283167 | — | — | 1 | 6.57 |
| CHEMBL4293342 | — | — | 1 | 6.51 |
| CHEMBL4294421 | — | — | 1 | 6.50 |
| CHEMBL4291024 | — | — | 1 | 6.39 |
| CHEMBL4288347 | — | — | 1 | 6.35 |
| CHEMBL4284218 | — | — | 1 | 6.29 |
| CHEMBL4294442 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4247249 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4282905 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4280317 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4294841 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4281138 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4287597 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4286811 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4279691 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4242494 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4277672 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4242551 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4294713 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4291768 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4288312 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4283167 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4293342 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4294421 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4291024 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4288347 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4284218 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4294442 | — | IC50 | = | 1300.0 | nM | 5.89 |