Assay Detail
Binding
CHEMBL5256647
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Inhibition of human recombinant cytoplasmic domain FGFR2 (8 to 134 residues) incubated for 120 mins by mobility shift assay
18
Total Activities
17
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 Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.34 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 2 | 9.00 |
| CHEMBL3701241 | — | — | 1 | 8.82 |
| CHEMBL3701243 | — | — | 1 | 8.47 |
| CHEMBL3701255 | — | — | 1 | 7.96 |
| CHEMBL5289003 | — | — | 1 | 7.77 |
| CHEMBL5278505 | — | — | 1 | 7.66 |
| CHEMBL5287545 | — | — | 1 | 7.54 |
| CHEMBL5269016 | — | — | 1 | 7.47 |
| CHEMBL5265881 | — | — | 1 | 7.24 |
| CHEMBL5268467 | — | — | 1 | 6.68 |
| CHEMBL5284165 | — | — | 1 | 6.68 |
| CHEMBL5273555 | — | — | 1 | 6.62 |
| CHEMBL3701282 | — | — | 1 | 6.61 |
| CHEMBL5272088 | — | — | 1 | 6.59 |
| CHEMBL5291403 | — | — | 1 | 6.50 |
| CHEMBL5275918 | — | — | 1 | 6.17 |
| CHEMBL5291034 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3701241 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3701243 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3701255 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5289003 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5278505 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5287545 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5269016 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5265881 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5284165 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL5268467 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL5273555 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL3701282 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL5272088 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL5291403 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL5275918 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL5291034 | — | IC50 | = | 2260.0 | nM | 5.65 |