Assay Detail
Binding
CHEMBL5541343
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FGFR3 K650M 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 | 8.03 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5592900 | — | — | 1 | 9.30 |
| CHEMBL5571671 | — | — | 1 | 8.60 |
| CHEMBL5566156 | — | — | 1 | 8.49 |
| CHEMBL5589734 | — | — | 1 | 8.48 |
| CHEMBL5572986 | — | — | 1 | 8.39 |
| CHEMBL5314537 | RESIGRATINIB | 2.0 | 1 | 8.36 |
| CHEMBL5594856 | — | — | 1 | 8.31 |
| CHEMBL5574600 | — | — | 1 | 8.29 |
| CHEMBL5572840 | — | — | 1 | 8.25 |
| CHEMBL5572491 | — | — | 1 | 8.15 |
| CHEMBL5572910 | — | — | 1 | 7.97 |
| CHEMBL5569299 | — | — | 1 | 7.75 |
| CHEMBL5563793 | — | — | 1 | 7.66 |
| CHEMBL5593760 | — | — | 1 | 7.51 |
| CHEMBL5568827 | — | — | 1 | 7.27 |
| CHEMBL5569392 | — | — | 1 | 6.96 |
| CHEMBL5566049 | — | — | 1 | 6.80 |
| CHEMBL5570727 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5592900 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5571671 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5566156 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5589734 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5572986 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5314537 | RESIGRATINIB | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5594856 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5574600 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5572840 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5572491 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5572910 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5569299 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL5563793 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL5593760 | — | IC50 | = | 30.6 | nM | 7.51 |
| CHEMBL5568827 | — | IC50 | = | 53.4 | nM | 7.27 |
| CHEMBL5569392 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5566049 | — | IC50 | = | 156.5 | nM | 6.80 |
| CHEMBL5570727 | — | IC50 | - | — | - |