Assay Detail
Binding
CHEMBL5581401
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Inhibition of FGFR2 (unknown origin)
7
Total Activities
7
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
Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2<sup>V564F</sup> gatekeeper mutation based on a pan-FGFR inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.85 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5589978 | — | — | 1 | 9.35 |
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 9.30 |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 1 | 8.89 |
| CHEMBL5594936 | — | — | 1 | 8.68 |
| CHEMBL3545376 | ERDAFITINIB | 4.0 | 1 | 8.60 |
| CHEMBL3828009 | LY-2874455 | 1.0 | 1 | 8.59 |
| CHEMBL5314555 | LIRAFUGRATINIB | 2.0 | 1 | 8.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5589978 | — | IC50 | = | 0.449 | nM | 9.35 |
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5594936 | — | IC50 | = | 2.09 | nM | 8.68 |
| CHEMBL3545376 | ERDAFITINIB | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3828009 | LY-2874455 | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5314555 | LIRAFUGRATINIB | IC50 | = | 3.1 | nM | 8.51 |