Assay Detail
Functional
CHEMBL1050131
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Antiproliferative activity against mouse Sal cells overexpressing IGF1R assessed as [3H]thymidine incorporation into DNA 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 of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.36 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575447 | — | — | 1 | 9.00 |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 8.15 |
| CHEMBL572581 | — | — | 1 | 7.62 |
| CHEMBL573246 | — | — | 1 | 7.41 |
| CHEMBL575888 | — | — | 1 | 7.33 |
| CHEMBL577385 | — | — | 1 | 7.17 |
| CHEMBL584355 | — | — | 1 | 7.16 |
| CHEMBL575681 | — | — | 1 | 6.88 |
| CHEMBL576179 | — | — | 1 | 6.51 |
| CHEMBL575669 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575447 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL575448 | BMS-754807 | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL572581 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL573246 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL575888 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL577385 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL584355 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL575681 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL576179 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL575669 | — | IC50 | = | 426.0 | nM | 6.37 |