Assay Detail
Binding
CHEMBL5541339
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FGFR2 N549H mutant (unknown origin) using 5-FAM-KKKKEEIYFFF-CONH2 peptide as fluorogenic substrate incubated for 80 mins in presence of ATP by fluorescence-based microfluidic mobility shift assay
18
Total Activities
18
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 KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.66 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5592900 | — | — | 1 | 8.44 |
| CHEMBL5594856 | — | — | 1 | 7.92 |
| CHEMBL5589734 | — | — | 1 | 7.88 |
| CHEMBL5574600 | — | — | 1 | 7.88 |
| CHEMBL5572910 | — | — | 1 | 7.81 |
| CHEMBL5571671 | — | — | 1 | 7.77 |
| CHEMBL5566156 | — | — | 1 | 7.75 |
| CHEMBL5572986 | — | — | 1 | 7.75 |
| CHEMBL5593760 | — | — | 1 | 7.73 |
| CHEMBL5572491 | — | — | 1 | 7.71 |
| CHEMBL5314537 | RESIGRATINIB | 2.0 | 1 | 7.63 |
| CHEMBL5569299 | — | — | 1 | 7.38 |
| CHEMBL5572840 | — | — | 1 | 7.33 |
| CHEMBL5568827 | — | — | 1 | 7.27 |
| CHEMBL5566049 | — | — | 1 | 6.59 |
| CHEMBL5570727 | — | — | 1 | - |
| CHEMBL5563793 | — | — | 1 | - |
| CHEMBL5569392 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5592900 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5594856 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5589734 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL5574600 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL5572910 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5571671 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL5566156 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL5572986 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL5593760 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL5572491 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL5314537 | RESIGRATINIB | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL5569299 | — | IC50 | = | 42.2 | nM | 7.38 |
| CHEMBL5572840 | — | IC50 | = | 46.6 | nM | 7.33 |
| CHEMBL5568827 | — | IC50 | = | 53.6 | nM | 7.27 |
| CHEMBL5566049 | — | IC50 | = | 256.1 | nM | 6.59 |
| CHEMBL5570727 | — | IC50 | - | — | - | |
| CHEMBL5563793 | — | IC50 | - | — | - | |
| CHEMBL5569392 | — | IC50 | - | — | - |