Assay Detail
Binding
CHEMBL5239771
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FGFR4 (unknown origin) using TK as substrate incubated for 1 hr in presence of biotin/ATP by HTRF assay
32
Total Activities
32
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 2-Amino-7-sulfonyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.06 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4514636 | FISOGATINIB | 2.0 | 1 | 8.28 |
| CHEMBL5290554 | — | — | 1 | 8.06 |
| CHEMBL5281307 | — | — | 1 | 7.98 |
| CHEMBL5283096 | — | — | 1 | 7.90 |
| CHEMBL5268351 | — | — | 1 | 7.86 |
| CHEMBL5280802 | — | — | 1 | 7.79 |
| CHEMBL5272254 | — | — | 1 | 7.77 |
| CHEMBL5278656 | — | — | 1 | 7.77 |
| CHEMBL5268564 | — | — | 1 | 7.54 |
| CHEMBL5275506 | — | — | 1 | 7.53 |
| CHEMBL5280110 | — | — | 1 | 7.48 |
| CHEMBL5267668 | — | — | 1 | 7.47 |
| CHEMBL5279776 | — | — | 1 | 7.43 |
| CHEMBL5283169 | — | — | 1 | 7.38 |
| CHEMBL5289886 | — | — | 1 | 7.32 |
| CHEMBL5290407 | — | — | 1 | 7.26 |
| CHEMBL5267788 | — | — | 1 | 7.22 |
| CHEMBL5276408 | — | — | 1 | 7.13 |
| CHEMBL5283222 | — | — | 1 | 6.95 |
| CHEMBL5265906 | — | — | 1 | 6.94 |
| CHEMBL5274760 | — | — | 1 | 6.90 |
| CHEMBL5288254 | — | — | 1 | 6.88 |
| CHEMBL5273517 | — | — | 1 | 6.70 |
| CHEMBL5290895 | — | — | 1 | 6.46 |
| CHEMBL5286749 | — | — | 1 | 6.21 |
| CHEMBL5274573 | — | — | 1 | 6.15 |
| CHEMBL5273832 | — | — | 1 | 6.05 |
| CHEMBL5291099 | — | — | 1 | 5.87 |
| CHEMBL5289858 | — | — | 1 | 5.70 |
| CHEMBL5269498 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514636 | FISOGATINIB | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5290554 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5281307 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5283096 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL5268351 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL5280802 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL5272254 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL5278656 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL5268564 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5275506 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL5280110 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5267668 | — | IC50 | = | 33.6 | nM | 7.47 |
| CHEMBL5279776 | — | IC50 | = | 36.8 | nM | 7.43 |
| CHEMBL5283169 | — | IC50 | = | 41.8 | nM | 7.38 |
| CHEMBL5289886 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL5290407 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5267788 | — | IC50 | = | 60.5 | nM | 7.22 |
| CHEMBL5276408 | — | IC50 | = | 74.7 | nM | 7.13 |
| CHEMBL5283222 | — | IC50 | = | 111.7 | nM | 6.95 |
| CHEMBL5265906 | — | IC50 | = | 113.9 | nM | 6.94 |
| CHEMBL5274760 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5288254 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5273517 | — | IC50 | = | 197.9 | nM | 6.70 |
| CHEMBL5290895 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL5286749 | — | IC50 | = | 614.5 | nM | 6.21 |
| CHEMBL5274573 | — | IC50 | = | 703.2 | nM | 6.15 |
| CHEMBL5273832 | — | IC50 | = | 892.7 | nM | 6.05 |
| CHEMBL5291099 | — | IC50 | = | 1343.0 | nM | 5.87 |
| CHEMBL5289858 | — | IC50 | = | 1975.0 | nM | 5.70 |
| CHEMBL5269498 | — | IC50 | = | 2195.0 | nM | 5.66 |
| CHEMBL5269015 | — | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL5288549 | — | IC50 | > | 10000.0 | nM | - |