Assay Detail
Functional
CHEMBL5541356
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Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RT-112 |
| Confidence | 1 — Organism |
| 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 | 6 | 7.27 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5571671 | — | — | 1 | 7.89 |
| CHEMBL5314537 | RESIGRATINIB | 2.0 | 1 | 7.79 |
| CHEMBL3545376 | ERDAFITINIB | 4.0 | 1 | 7.41 |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 1 | 7.13 |
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 6.76 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5571671 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL5314537 | RESIGRATINIB | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL3545376 | ERDAFITINIB | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 74.3 | nM | 7.13 |
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 218.0 | nM | 6.66 |