Assay Detail
Binding
CHEMBL866816
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR2
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.21 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL209555 | — | — | 1 | 7.85 |
| CHEMBL384909 | — | — | 1 | 7.77 |
| CHEMBL365318 | — | — | 1 | 7.75 |
| CHEMBL377734 | — | — | 1 | 7.64 |
| CHEMBL379370 | — | — | 1 | 7.54 |
| CHEMBL212304 | — | — | 1 | 7.52 |
| CHEMBL208788 | — | — | 1 | 7.19 |
| CHEMBL212267 | — | — | 1 | 7.15 |
| CHEMBL379661 | — | — | 1 | 7.13 |
| CHEMBL211060 | — | — | 1 | 7.07 |
| CHEMBL379320 | — | — | 1 | 7.06 |
| CHEMBL208911 | — | — | 1 | 6.96 |
| CHEMBL207520 | — | — | 1 | 6.55 |
| CHEMBL379495 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL209555 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL384909 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL365318 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL377734 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL379370 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL212304 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL208788 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL212267 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL379661 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL211060 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL379320 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL208911 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL207520 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL379495 | — | IC50 | = | 1900.0 | nM | 5.72 |