Assay Detail
Binding
CHEMBL5581404
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Inhibition of FGFR3 (unknown origin)
6
Total Activities
6
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 | 6 | 8.32 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 8.92 |
| CHEMBL5589978 | — | — | 1 | 8.90 |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 1 | 8.80 |
| CHEMBL3545376 | ERDAFITINIB | 4.0 | 1 | 8.52 |
| CHEMBL3828009 | LY-2874455 | 1.0 | 1 | 8.19 |
| CHEMBL5314555 | LIRAFUGRATINIB | 2.0 | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5589978 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3545376 | ERDAFITINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3828009 | LY-2874455 | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5314555 | LIRAFUGRATINIB | IC50 | = | 274.0 | nM | 6.56 |