Assay Detail
Binding
CHEMBL5541337
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type FGFR1 (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 | 8.33 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5592900 | — | — | 1 | 9.00 |
| CHEMBL5593760 | — | — | 1 | 8.82 |
| CHEMBL5589734 | — | — | 1 | 8.59 |
| CHEMBL5574600 | — | — | 1 | 8.52 |
| CHEMBL5566156 | — | — | 1 | 8.49 |
| CHEMBL5571671 | — | — | 1 | 8.48 |
| CHEMBL5563793 | — | — | 1 | 8.44 |
| CHEMBL5314537 | RESIGRATINIB | 2.0 | 1 | 8.42 |
| CHEMBL5572910 | — | — | 1 | 8.38 |
| CHEMBL5594856 | — | — | 1 | 8.37 |
| CHEMBL5572491 | — | — | 1 | 8.35 |
| CHEMBL5568827 | — | — | 1 | 8.29 |
| CHEMBL5572986 | — | — | 1 | 8.22 |
| CHEMBL5569299 | — | — | 1 | 8.15 |
| CHEMBL5572840 | — | — | 1 | 8.01 |
| CHEMBL5570727 | — | — | 1 | 7.85 |
| CHEMBL5566049 | — | — | 1 | 7.82 |
| CHEMBL5569392 | — | — | 1 | 7.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5592900 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5593760 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5589734 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5574600 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5566156 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5571671 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5563793 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5314537 | RESIGRATINIB | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5572910 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5594856 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5572491 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5568827 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5572986 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5569299 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5572840 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5570727 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL5566049 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL5569392 | — | IC50 | = | 15.4 | nM | 7.81 |