Assay Detail
Binding
CHEMBL4043779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His-tagged FGFR3 cytoplasmic domain (399 to 806 residues) expressed in baculovirus using Tyr-4 peptide after 1 hr by FRET-based Z'-Lyte assay
14
Total Activities
14
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
2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.07 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100258 | — | — | 1 | 8.29 |
| CHEMBL4092508 | — | — | 1 | 8.29 |
| CHEMBL4096041 | — | — | 1 | 8.27 |
| CHEMBL2216830 | — | — | 1 | 8.22 |
| CHEMBL4079538 | — | — | 1 | 8.15 |
| CHEMBL4103795 | — | — | 1 | 8.15 |
| CHEMBL4068733 | — | — | 1 | 8.15 |
| CHEMBL4092354 | — | — | 1 | 8.12 |
| CHEMBL4088313 | — | — | 1 | 7.96 |
| CHEMBL4077029 | — | — | 1 | 7.94 |
| CHEMBL4069509 | — | — | 1 | 7.89 |
| CHEMBL4060079 | — | — | 1 | 7.79 |
| CHEMBL4096738 | — | — | 1 | 7.69 |
| CHEMBL4084614 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100258 | — | IC50 | = | 5.09 | nM | 8.29 |
| CHEMBL4092508 | — | IC50 | = | 5.07 | nM | 8.29 |
| CHEMBL4096041 | — | IC50 | = | 5.38 | nM | 8.27 |
| CHEMBL2216830 | — | IC50 | = | 5.99 | nM | 8.22 |
| CHEMBL4079538 | — | IC50 | = | 7.04 | nM | 8.15 |
| CHEMBL4103795 | — | IC50 | = | 7.12 | nM | 8.15 |
| CHEMBL4068733 | — | IC50 | = | 7.15 | nM | 8.15 |
| CHEMBL4092354 | — | IC50 | = | 7.59 | nM | 8.12 |
| CHEMBL4088313 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL4077029 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL4069509 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL4060079 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL4096738 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL4084614 | — | IC50 | > | 1000.0 | nM | - |