Assay Detail
Binding
CHEMBL5135717
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type FGFR1 (unknown origin) by radiometric kinase activity assay
9
Total Activities
9
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
Identification of Pyridinyltriazine Derivatives as Potent panFGFR Inhibitors against Gatekeeper Mutants for Overcoming Drug Resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.66 | 8.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545376 | ERDAFITINIB | 4.0 | 1 | 8.81 |
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 8.73 |
| CHEMBL5194218 | — | — | 1 | 8.43 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | - |
| CHEMBL5179166 | — | — | 1 | - |
| CHEMBL5177100 | — | — | 1 | - |
| CHEMBL5198569 | — | — | 1 | - |
| CHEMBL5193966 | — | — | 1 | - |
| CHEMBL5181852 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545376 | ERDAFITINIB | IC50 | = | 1.53 | nM | 8.81 |
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 1.88 | nM | 8.73 |
| CHEMBL5194218 | — | IC50 | = | 3.68 | nM | 8.43 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | < | 0.5 | nM | - |
| CHEMBL5179166 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5177100 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5198569 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5193966 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL5181852 | — | IC50 | < | 0.5 | nM | - |