Assay Detail
Binding
CHEMBL3861870
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Inhibition of human FGFR1 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 |
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 | 7.44 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3984621 | — | — | 1 | 8.92 |
| CHEMBL3681278 | — | — | 1 | 8.82 |
| CHEMBL3891894 | — | — | 1 | 8.54 |
| CHEMBL3681287 | — | — | 1 | 8.54 |
| CHEMBL3681314 | — | — | 1 | 8.52 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | 8.03 |
| CHEMBL3895337 | — | — | 1 | 7.75 |
| CHEMBL3934547 | — | — | 1 | 7.48 |
| CHEMBL3676329 | — | — | 1 | 7.31 |
| CHEMBL3681244 | — | — | 1 | 7.30 |
| CHEMBL3681317 | — | — | 1 | 7.25 |
| CHEMBL3959997 | — | — | 1 | 7.16 |
| CHEMBL3976548 | — | — | 1 | 6.89 |
| CHEMBL3941474 | — | — | 1 | 6.80 |
| CHEMBL3981956 | — | — | 1 | 6.57 |
| CHEMBL3947281 | — | — | 1 | 6.35 |
| CHEMBL3956001 | — | — | 1 | 5.96 |
| CHEMBL3905685 | — | — | 1 | 5.72 |
| CHEMBL3952373 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3984621 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3681278 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3891894 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3681287 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3681314 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL3895337 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3934547 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3676329 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3681244 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3681317 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3959997 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3976548 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3941474 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3981956 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3947281 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3956001 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3905685 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3952373 | — | IC50 | > | 50000.0 | nM | - |