Assay Detail
Binding
CHEMBL971608
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human IGF1R expressed in transgenic mouse IGFSal cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IGFSal |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.57 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460997 | — | — | 1 | 7.75 |
| CHEMBL468671 | — | — | 1 | 7.75 |
| CHEMBL469292 | — | — | 1 | 7.70 |
| CHEMBL461198 | — | — | 1 | 7.66 |
| CHEMBL512126 | — | — | 1 | 7.64 |
| CHEMBL460996 | — | — | 1 | 7.60 |
| CHEMBL461422 | — | — | 1 | 7.58 |
| CHEMBL468672 | — | — | 1 | 7.51 |
| CHEMBL459729 | — | — | 1 | 7.47 |
| CHEMBL401930 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460997 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL468671 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL469292 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL461198 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL512126 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL460996 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL461422 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL468672 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL459729 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL401930 | — | IC50 | = | 100.0 | nM | 7.00 |