Assay Detail
Functional
CHEMBL971607
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Antiproliferative activity against transgenic mouse SAL cells overexpressing human IGF1R assessed as [3H]thymidine incorporation after 72 hrs
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | SAL |
| Confidence | 1 — Organism |
| 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 | 7.06 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512126 | — | — | 1 | 7.89 |
| CHEMBL469292 | — | — | 1 | 7.40 |
| CHEMBL460997 | — | — | 1 | 7.34 |
| CHEMBL468672 | — | — | 1 | 7.12 |
| CHEMBL461198 | — | — | 1 | 7.07 |
| CHEMBL401930 | — | — | 1 | 6.96 |
| CHEMBL461422 | — | — | 1 | 6.79 |
| CHEMBL459729 | — | — | 1 | 6.73 |
| CHEMBL468671 | — | — | 1 | 6.66 |
| CHEMBL460996 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512126 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL469292 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL460997 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL468672 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL461198 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL401930 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL461422 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL459729 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL468671 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL460996 | — | IC50 | = | 241.0 | nM | 6.62 |