Assay Detail
Binding
CHEMBL5736328
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Measurement of Inhibitory Effect on FGFR3 Kinase Activity: The inhibitory effect of the compounds on FGFR3 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. The final concentration of ATP was 50 μM.
21
Total Activities
6
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Antitumor drug for intermittent administration of FGFR inhibitor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 9.45 | 10.00 |
| kon | 7 | - | - |
| k_off | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3701241 | — | — | 6 | 10.00 |
| CHEMBL3701239 | — | — | 3 | 9.70 |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 3 | 9.30 |
| CHEMBL3701262 | — | — | 3 | 9.30 |
| CHEMBL3701267 | — | — | 3 | 9.15 |
| CHEMBL3701275 | — | — | 3 | 9.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3701241 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3701239 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3701241 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3701262 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3701275 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3701267 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3701238 | FUTIBATINIB | kon | = | - | — | - |
| CHEMBL3701238 | FUTIBATINIB | k_off | = | - | s-1 | - |
| CHEMBL3701239 | — | kon | = | - | — | - |
| CHEMBL3701239 | — | k_off | = | - | s-1 | - |
| CHEMBL3701241 | — | kon | = | - | — | - |
| CHEMBL3701241 | — | k_off | = | - | s-1 | - |
| CHEMBL3701262 | — | k_off | = | - | s-1 | - |
| CHEMBL3701241 | — | kon | = | - | — | - |
| CHEMBL3701241 | — | k_off | = | - | s-1 | - |
| CHEMBL3701267 | — | kon | = | - | — | - |
| CHEMBL3701267 | — | k_off | = | - | s-1 | - |
| CHEMBL3701275 | — | kon | = | - | — | - |
| CHEMBL3701275 | — | k_off | = | - | s-1 | - |
| CHEMBL3701262 | — | kon | = | - | — | - |