Assay Detail
Binding
CHEMBL4265765
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ACAT in human J774A.1 cells assessed as reduction in esterified-cholesterol accumulation after 18 hrs in presence of 25-hydroxycholesterol by cholesterol E-test analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| 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 | 6.63 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4281138 | — | — | 1 | 8.52 |
| CHEMBL4247249 | — | — | 1 | 8.15 |
| CHEMBL4282905 | — | — | 1 | 8.05 |
| CHEMBL4288347 | — | — | 1 | 7.58 |
| CHEMBL4291768 | — | — | 1 | 7.00 |
| CHEMBL4280317 | — | — | 1 | 6.77 |
| CHEMBL4287597 | — | — | 1 | 6.60 |
| CHEMBL4283167 | — | — | 1 | 6.60 |
| CHEMBL4294841 | — | — | 1 | 6.58 |
| CHEMBL4284218 | — | — | 1 | 6.55 |
| CHEMBL4277672 | — | — | 1 | 6.43 |
| CHEMBL4294442 | — | — | 1 | 6.43 |
| CHEMBL4293342 | — | — | 1 | 6.39 |
| CHEMBL4279691 | — | — | 1 | 6.37 |
| CHEMBL4294421 | — | — | 1 | 6.35 |
| CHEMBL4291024 | — | — | 1 | 6.31 |
| CHEMBL4242494 | — | — | 1 | 6.09 |
| CHEMBL4288312 | — | — | 1 | 5.92 |
| CHEMBL4286811 | — | — | 1 | 5.80 |
| CHEMBL4294713 | — | — | 1 | 5.57 |
| CHEMBL4242551 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4281138 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4247249 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4282905 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4288347 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4291768 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4280317 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4287597 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4283167 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4294841 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4284218 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4277672 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4294442 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4293342 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4279691 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4294421 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4291024 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4242494 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4288312 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4286811 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4294713 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4242551 | — | IC50 | = | 5600.0 | nM | 5.25 |