Assay Detail
Binding
CHEMBL5033055
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human FGFR3 (450 to 758 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay
42
Total Activities
42
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 and Optimization of a Novel 2<i>H</i>-Pyrazolo[3,4-d]pyrimidine Derivative as a Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.05 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 1 | 9.28 |
| CHEMBL5088737 | — | — | 1 | 9.05 |
| CHEMBL3348846 | FEXAGRATINIB | 2.0 | 1 | 8.74 |
| CHEMBL5084546 | — | — | 1 | 8.56 |
| CHEMBL5091141 | — | — | 1 | 8.47 |
| CHEMBL5077247 | — | — | 1 | 7.99 |
| CHEMBL5078278 | — | — | 1 | 7.95 |
| CHEMBL5086846 | — | — | 1 | 7.91 |
| CHEMBL5082785 | — | — | 1 | 7.88 |
| CHEMBL5084840 | — | — | 1 | 7.81 |
| CHEMBL5086719 | — | — | 1 | 7.65 |
| CHEMBL5070239 | — | — | 1 | 7.01 |
| CHEMBL5080570 | — | — | 1 | 6.94 |
| CHEMBL5088036 | — | — | 1 | 6.88 |
| CHEMBL5073763 | — | — | 1 | 6.50 |
| CHEMBL5075228 | — | — | 1 | 6.49 |
| CHEMBL5090652 | — | — | 1 | 6.47 |
| CHEMBL5078978 | — | — | 1 | 6.46 |
| CHEMBL5078797 | — | — | 1 | 6.43 |
| CHEMBL5089372 | — | — | 1 | 6.38 |
| CHEMBL5082994 | — | — | 1 | 6.31 |
| CHEMBL5090807 | — | — | 1 | 6.28 |
| CHEMBL5092310 | — | — | 1 | 6.28 |
| CHEMBL5093158 | — | — | 1 | 6.28 |
| CHEMBL5082464 | — | — | 1 | 6.28 |
| CHEMBL5089648 | — | — | 1 | 6.24 |
| CHEMBL5074413 | — | — | 1 | 6.14 |
| CHEMBL5088944 | — | — | 1 | 6.11 |
| CHEMBL5094622 | — | — | 1 | 6.06 |
| CHEMBL5079163 | — | — | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL5088737 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3348846 | FEXAGRATINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5084546 | — | IC50 | = | 2.74 | nM | 8.56 |
| CHEMBL5091141 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5077247 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5078278 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL5086846 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5082785 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL5084840 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5086719 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL5070239 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5080570 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5088036 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5073763 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL5075228 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL5090652 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL5078978 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL5078797 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL5089372 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL5082994 | — | IC50 | = | 486.0 | nM | 6.31 |
| CHEMBL5090807 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL5082464 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5092310 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL5093158 | — | IC50 | = | 521.0 | nM | 6.28 |
| CHEMBL5089648 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5074413 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL5088944 | — | IC50 | = | 769.0 | nM | 6.11 |
| CHEMBL5094622 | — | IC50 | = | 875.0 | nM | 6.06 |
| CHEMBL5079163 | — | IC50 | = | 1321.0 | nM | 5.88 |
| CHEMBL5072738 | — | IC50 | = | 1978.0 | nM | 5.70 |
| CHEMBL5081042 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5084946 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5080177 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5076725 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5088393 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5075780 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5080128 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5083817 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5092355 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5071691 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5081683 | — | IC50 | > | 10.0 | nM | - |