Assay Detail
Binding
CHEMBL3861875
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SRC 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
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| 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 | 6.63 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3976548 | — | — | 1 | 9.74 |
| CHEMBL3984621 | — | — | 1 | 9.37 |
| CHEMBL3981956 | — | — | 1 | 8.37 |
| CHEMBL3956001 | — | — | 1 | 7.96 |
| CHEMBL3947281 | — | — | 1 | 7.51 |
| CHEMBL3941474 | — | — | 1 | 6.64 |
| CHEMBL3905685 | — | — | 1 | 6.60 |
| CHEMBL3681278 | — | — | 1 | 6.52 |
| CHEMBL3959997 | — | — | 1 | 6.48 |
| CHEMBL3681314 | — | — | 1 | 6.41 |
| CHEMBL3891894 | — | — | 1 | 6.29 |
| CHEMBL3934547 | — | — | 1 | 5.70 |
| CHEMBL3895337 | — | — | 1 | 5.47 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | 5.23 |
| CHEMBL3681317 | — | — | 1 | 5.16 |
| CHEMBL3681287 | — | — | 1 | 4.80 |
| CHEMBL3952373 | — | — | 1 | 4.48 |
| CHEMBL3676329 | — | — | 1 | - |
| CHEMBL3681244 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3976548 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3984621 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL3981956 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3956001 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3947281 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3941474 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3905685 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3681278 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3959997 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3681314 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3891894 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3934547 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3895337 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3681317 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3681287 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3952373 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3676329 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3681244 | — | IC50 | > | 50000.0 | nM | - |