Assay Detail
Binding
CHEMBL4043780
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His-tagged FGFR4 cytoplasmic domain (781 to 1338 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 | 6.83 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4079538 | — | — | 1 | 7.36 |
| CHEMBL4068733 | — | — | 1 | 7.32 |
| CHEMBL4096041 | — | — | 1 | 7.16 |
| CHEMBL4092508 | — | — | 1 | 7.11 |
| CHEMBL4096738 | — | — | 1 | 7.10 |
| CHEMBL4060079 | — | — | 1 | 6.78 |
| CHEMBL4088313 | — | — | 1 | 6.75 |
| CHEMBL4103795 | — | — | 1 | 6.73 |
| CHEMBL2216830 | — | — | 1 | 6.58 |
| CHEMBL4100258 | — | — | 1 | 6.57 |
| CHEMBL4069509 | — | — | 1 | 6.53 |
| CHEMBL4077029 | — | — | 1 | 6.42 |
| CHEMBL4092354 | — | — | 1 | 6.34 |
| CHEMBL4084614 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4079538 | — | IC50 | = | 44.2 | nM | 7.36 |
| CHEMBL4068733 | — | IC50 | = | 47.8 | nM | 7.32 |
| CHEMBL4096041 | — | IC50 | = | 68.7 | nM | 7.16 |
| CHEMBL4092508 | — | IC50 | = | 78.1 | nM | 7.11 |
| CHEMBL4096738 | — | IC50 | = | 79.2 | nM | 7.10 |
| CHEMBL4060079 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL4088313 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4103795 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL2216830 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL4100258 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL4069509 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL4077029 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL4092354 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL4084614 | — | IC50 | > | 1000.0 | nM | - |