Assay Detail
Functional
CHEMBL5581420
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human MDA-MB-231 cells expressing FGFR1 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 1 — Organism |
| 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 | 2 | 5.75 | 5.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | 1.0 | 1 | 5.90 |
| CHEMBL5589978 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | IC50 | = | 1253.0 | nM | 5.90 |
| CHEMBL5589978 | — | IC50 | = | 2522.0 | nM | 5.60 |