Assay Detail
Binding
CHEMBL3861874
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human KDR by time-resolved fluorescence or time-resolved fluorescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.54 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3984621 | — | — | 1 | 8.62 |
| CHEMBL3959997 | — | — | 1 | 8.19 |
| CHEMBL3976548 | — | — | 1 | 7.55 |
| CHEMBL3941474 | — | — | 1 | 7.28 |
| CHEMBL3681278 | — | — | 1 | 6.92 |
| CHEMBL3981956 | — | — | 1 | 6.77 |
| CHEMBL3891894 | — | — | 1 | 6.68 |
| CHEMBL3681314 | — | — | 1 | 6.55 |
| CHEMBL3676329 | — | — | 1 | 6.54 |
| CHEMBL3934547 | — | — | 1 | 6.47 |
| CHEMBL3895337 | — | — | 1 | 6.43 |
| CHEMBL3956001 | — | — | 1 | 6.39 |
| CHEMBL3681317 | — | — | 1 | 6.00 |
| CHEMBL3947281 | — | — | 1 | 5.80 |
| CHEMBL3681287 | — | — | 1 | 5.77 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | 5.68 |
| CHEMBL3952373 | — | — | 1 | 5.57 |
| CHEMBL3905685 | — | — | 1 | 5.54 |
| CHEMBL3681244 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3984621 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3959997 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3976548 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3941474 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3681278 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3981956 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3891894 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3681314 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3676329 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3934547 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3895337 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3956001 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3681317 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3947281 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3681287 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3952373 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3905685 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3681244 | — | IC50 | = | 3400.0 | nM | 5.47 |