Assay Detail
Binding
CHEMBL4043778
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant cytoplasmic His-tagged FGFR2 (403 to 822 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 | 8.57 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096041 | — | — | 1 | 9.08 |
| CHEMBL4100258 | — | — | 1 | 8.92 |
| CHEMBL4088313 | — | — | 1 | 8.86 |
| CHEMBL4092508 | — | — | 1 | 8.84 |
| CHEMBL4068733 | — | — | 1 | 8.80 |
| CHEMBL4092354 | — | — | 1 | 8.79 |
| CHEMBL4103795 | — | — | 1 | 8.78 |
| CHEMBL4079538 | — | — | 1 | 8.75 |
| CHEMBL2216830 | — | — | 1 | 8.64 |
| CHEMBL4060079 | — | — | 1 | 8.62 |
| CHEMBL4069509 | — | — | 1 | 8.58 |
| CHEMBL4077029 | — | — | 1 | 8.56 |
| CHEMBL4096738 | — | — | 1 | 8.44 |
| CHEMBL4084614 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096041 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL4100258 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL4088313 | — | IC50 | = | 1.39 | nM | 8.86 |
| CHEMBL4092508 | — | IC50 | = | 1.45 | nM | 8.84 |
| CHEMBL4068733 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL4092354 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL4103795 | — | IC50 | = | 1.65 | nM | 8.78 |
| CHEMBL4079538 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL2216830 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL4060079 | — | IC50 | = | 2.39 | nM | 8.62 |
| CHEMBL4069509 | — | IC50 | = | 2.61 | nM | 8.58 |
| CHEMBL4077029 | — | IC50 | = | 2.73 | nM | 8.56 |
| CHEMBL4096738 | — | IC50 | = | 3.63 | nM | 8.44 |
| CHEMBL4084614 | — | IC50 | = | 414.0 | nM | 6.38 |