Assay Detail
Binding
CHEMBL5541340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FGFR2 V564F 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 | 7.68 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5571671 | — | — | 1 | 8.62 |
| CHEMBL5572840 | — | — | 1 | 8.26 |
| CHEMBL5592900 | — | — | 1 | 8.24 |
| CHEMBL5589734 | — | — | 1 | 8.21 |
| CHEMBL5566156 | — | — | 1 | 8.16 |
| CHEMBL5574600 | — | — | 1 | 8.00 |
| CHEMBL5572491 | — | — | 1 | 7.82 |
| CHEMBL5568827 | — | — | 1 | 7.79 |
| CHEMBL5314537 | RESIGRATINIB | 2.0 | 1 | 7.76 |
| CHEMBL5572986 | — | — | 1 | 7.66 |
| CHEMBL5572910 | — | — | 1 | 7.62 |
| CHEMBL5593760 | — | — | 1 | 7.60 |
| CHEMBL5594856 | — | — | 1 | 7.50 |
| CHEMBL5563793 | — | — | 1 | 7.43 |
| CHEMBL5569299 | — | — | 1 | 7.14 |
| CHEMBL5570727 | — | — | 1 | 7.10 |
| CHEMBL5569392 | — | — | 1 | 6.78 |
| CHEMBL5566049 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5571671 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5572840 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5592900 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5589734 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5566156 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5574600 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL5572491 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL5568827 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL5314537 | RESIGRATINIB | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL5572986 | — | IC50 | = | 21.9 | nM | 7.66 |
| CHEMBL5572910 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL5593760 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL5594856 | — | IC50 | = | 31.9 | nM | 7.50 |
| CHEMBL5563793 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL5569299 | — | IC50 | = | 72.1 | nM | 7.14 |
| CHEMBL5570727 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5569392 | — | IC50 | = | 164.8 | nM | 6.78 |
| CHEMBL5566049 | — | IC50 | = | 295.3 | nM | 6.53 |