Assay Detail
Functional
CHEMBL5581387
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against FGFR2 amplified human KATO III cells measured after 3 days by MTT assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KATO III |
| 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 | 26 | 7.97 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | 1.0 | 1 | 9.15 |
| CHEMBL5589978 | — | — | 1 | 9.10 |
| CHEMBL5583689 | — | — | 1 | 8.38 |
| CHEMBL5593563 | — | — | 1 | 8.31 |
| CHEMBL5590906 | — | — | 1 | 8.17 |
| CHEMBL5593094 | — | — | 1 | 8.14 |
| CHEMBL5592678 | — | — | 1 | 8.09 |
| CHEMBL5591134 | — | — | 1 | 7.99 |
| CHEMBL5593143 | — | — | 1 | 7.98 |
| CHEMBL5593940 | — | — | 1 | 7.92 |
| CHEMBL5593805 | — | — | 1 | 7.83 |
| CHEMBL5595564 | — | — | 1 | 7.81 |
| CHEMBL5595539 | — | — | 1 | 7.76 |
| CHEMBL5594962 | — | — | 1 | 7.70 |
| CHEMBL5592450 | — | — | 1 | 7.65 |
| CHEMBL5590542 | — | — | 1 | 7.41 |
| CHEMBL5595449 | — | — | 1 | 7.38 |
| CHEMBL5595375 | — | — | 1 | 7.33 |
| CHEMBL5595234 | — | — | 1 | 7.33 |
| CHEMBL5584007 | — | — | 1 | - |
| CHEMBL5595769 | — | — | 1 | - |
| CHEMBL5590532 | — | — | 1 | - |
| CHEMBL5594216 | — | — | 1 | - |
| CHEMBL5593470 | — | — | 1 | - |
| CHEMBL5592393 | — | — | 1 | - |
| CHEMBL5594667 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL5589978 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL5583689 | — | IC50 | = | 4.16 | nM | 8.38 |
| CHEMBL5593563 | — | IC50 | = | 4.93 | nM | 8.31 |
| CHEMBL5590906 | — | IC50 | = | 6.83 | nM | 8.17 |
| CHEMBL5593094 | — | IC50 | = | 7.29 | nM | 8.14 |
| CHEMBL5592678 | — | IC50 | = | 8.08 | nM | 8.09 |
| CHEMBL5591134 | — | IC50 | = | 10.14 | nM | 7.99 |
| CHEMBL5593143 | — | IC50 | = | 10.41 | nM | 7.98 |
| CHEMBL5593940 | — | IC50 | = | 12.05 | nM | 7.92 |
| CHEMBL5593805 | — | IC50 | = | 14.85 | nM | 7.83 |
| CHEMBL5595564 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL5595539 | — | IC50 | = | 17.54 | nM | 7.76 |
| CHEMBL5594962 | — | IC50 | = | 19.97 | nM | 7.70 |
| CHEMBL5592450 | — | IC50 | = | 22.36 | nM | 7.65 |
| CHEMBL5590542 | — | IC50 | = | 39.24 | nM | 7.41 |
| CHEMBL5595449 | — | IC50 | = | 41.8 | nM | 7.38 |
| CHEMBL5595375 | — | IC50 | = | 46.57 | nM | 7.33 |
| CHEMBL5595234 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5584007 | — | IC50 | > | 50.0 | nM | - |
| CHEMBL5595769 | — | IC50 | > | 50.0 | nM | - |
| CHEMBL5590532 | — | IC50 | > | 50.0 | nM | - |
| CHEMBL5594216 | — | IC50 | > | 50.0 | nM | - |
| CHEMBL5593470 | — | IC50 | > | 50.0 | nM | - |
| CHEMBL5592393 | — | IC50 | > | 50.0 | nM | - |
| CHEMBL5594667 | — | IC50 | > | 50.0 | nM | - |