Assay Detail
ADMET
CHEMBL971609
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Inhibition of human recombinant CYP3A4 in human liver microsomes using BFC as a substrate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.01 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL401930 | — | — | 1 | 7.30 |
| CHEMBL512126 | — | — | 1 | 5.11 |
| CHEMBL469292 | — | — | 1 | 5.00 |
| CHEMBL468671 | — | — | 1 | 4.96 |
| CHEMBL461198 | — | — | 1 | 4.85 |
| CHEMBL460997 | — | — | 1 | 4.71 |
| CHEMBL460996 | — | — | 1 | 4.64 |
| CHEMBL459729 | — | — | 1 | 4.58 |
| CHEMBL468672 | — | — | 1 | 4.55 |
| CHEMBL461422 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL401930 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL512126 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL469292 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL468671 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL461198 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL460997 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL460996 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL459729 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL468672 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL461422 | — | IC50 | = | 40000.0 | nM | 4.40 |