Assay Detail
Binding
CHEMBL4043777
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His-tagged FGFR1 cytoplasmic domain (308 to 731 residues) expressed in baculovirus using Tyr-4 peptide after 1 hr by FRET-based Z'-Lyte assay
23
Total Activities
23
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 | 23 | 8.70 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100258 | — | — | 1 | 9.55 |
| CHEMBL4092354 | — | — | 1 | 9.14 |
| CHEMBL4077029 | — | — | 1 | 9.04 |
| CHEMBL4092508 | — | — | 1 | 9.00 |
| CHEMBL4096041 | — | — | 1 | 8.97 |
| CHEMBL4069509 | — | — | 1 | 8.97 |
| CHEMBL4088313 | — | — | 1 | 8.97 |
| CHEMBL4103795 | — | — | 1 | 8.94 |
| CHEMBL4068733 | — | — | 1 | 8.93 |
| CHEMBL4079538 | — | — | 1 | 8.92 |
| CHEMBL4096738 | — | — | 1 | 8.91 |
| CHEMBL4060079 | — | — | 1 | 8.88 |
| CHEMBL4102560 | — | — | 1 | 8.75 |
| CHEMBL4066038 | — | — | 1 | 8.74 |
| CHEMBL4072483 | — | — | 1 | 8.71 |
| CHEMBL4099403 | — | — | 1 | 8.64 |
| CHEMBL4061908 | — | — | 1 | 8.63 |
| CHEMBL4100110 | — | — | 1 | 8.51 |
| CHEMBL4064676 | — | — | 1 | 8.45 |
| CHEMBL2216830 | — | — | 1 | 8.44 |
| CHEMBL4087420 | — | — | 1 | 8.34 |
| CHEMBL4073261 | — | — | 1 | 7.97 |
| CHEMBL4084614 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100258 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4092354 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4077029 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL4092508 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL4096041 | — | IC50 | = | 1.06 | nM | 8.97 |
| CHEMBL4069509 | — | IC50 | = | 1.07 | nM | 8.97 |
| CHEMBL4088313 | — | IC50 | = | 1.06 | nM | 8.97 |
| CHEMBL4103795 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL4068733 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL4079538 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL4096738 | — | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL4060079 | — | IC50 | = | 1.32 | nM | 8.88 |
| CHEMBL4102560 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL4066038 | — | IC50 | = | 1.81 | nM | 8.74 |
| CHEMBL4072483 | — | IC50 | = | 1.97 | nM | 8.71 |
| CHEMBL4099403 | — | IC50 | = | 2.28 | nM | 8.64 |
| CHEMBL4061908 | — | IC50 | = | 2.33 | nM | 8.63 |
| CHEMBL4100110 | — | IC50 | = | 3.08 | nM | 8.51 |
| CHEMBL4064676 | — | IC50 | = | 3.54 | nM | 8.45 |
| CHEMBL2216830 | — | IC50 | = | 3.65 | nM | 8.44 |
| CHEMBL4087420 | — | IC50 | = | 4.59 | nM | 8.34 |
| CHEMBL4073261 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL4084614 | — | IC50 | = | 200.0 | nM | 6.70 |