Assay Detail
Binding
CHEMBL5541342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FGFR3 V555M 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 | 7.22 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5571671 | — | — | 1 | 8.04 |
| CHEMBL5592900 | — | — | 1 | 7.88 |
| CHEMBL5589734 | — | — | 1 | 7.80 |
| CHEMBL5568827 | — | — | 1 | 7.70 |
| CHEMBL5566156 | — | — | 1 | 7.58 |
| CHEMBL5314537 | RESIGRATINIB | 2.0 | 1 | 7.56 |
| CHEMBL5572491 | — | — | 1 | 7.52 |
| CHEMBL5572840 | — | — | 1 | 7.27 |
| CHEMBL5574600 | — | — | 1 | 7.27 |
| CHEMBL5593760 | — | — | 1 | 6.96 |
| CHEMBL5563793 | — | — | 1 | 6.96 |
| CHEMBL5572986 | — | — | 1 | 6.94 |
| CHEMBL5572910 | — | — | 1 | 6.89 |
| CHEMBL5594856 | — | — | 1 | 6.67 |
| CHEMBL5566049 | — | — | 1 | 6.58 |
| CHEMBL5570727 | — | — | 1 | 6.54 |
| CHEMBL5569299 | — | — | 1 | 6.51 |
| CHEMBL5569392 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5571671 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL5592900 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL5589734 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5568827 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5566156 | — | IC50 | = | 26.6 | nM | 7.58 |
| CHEMBL5314537 | RESIGRATINIB | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL5572491 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5572840 | — | IC50 | = | 54.1 | nM | 7.27 |
| CHEMBL5574600 | — | IC50 | = | 53.6 | nM | 7.27 |
| CHEMBL5593760 | — | IC50 | = | 109.4 | nM | 6.96 |
| CHEMBL5563793 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5572986 | — | IC50 | = | 113.7 | nM | 6.94 |
| CHEMBL5572910 | — | IC50 | = | 129.2 | nM | 6.89 |
| CHEMBL5594856 | — | IC50 | = | 215.4 | nM | 6.67 |
| CHEMBL5566049 | — | IC50 | = | 265.6 | nM | 6.58 |
| CHEMBL5570727 | — | IC50 | = | 288.7 | nM | 6.54 |
| CHEMBL5569299 | — | IC50 | = | 306.8 | nM | 6.51 |
| CHEMBL5569392 | — | IC50 | > | 1000.0 | nM | - |