Assay Detail
Functional
CHEMBL5583178
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Inhibition of cell viability in human RT112/84 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RT112/84 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.91 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545376 | ERDAFITINIB | 4.0 | 1 | 8.44 |
| CHEMBL5595947 | — | — | 1 | 8.08 |
| CHEMBL5595500 | — | — | 1 | 8.05 |
| CHEMBL5593800 | — | — | 1 | 8.04 |
| CHEMBL5592211 | — | — | 1 | 7.89 |
| CHEMBL5590817 | — | — | 1 | 7.82 |
| CHEMBL5584069 | — | — | 1 | 7.57 |
| CHEMBL5592556 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545376 | ERDAFITINIB | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5595947 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5595500 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5593800 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5592211 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5590817 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5584069 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5592556 | — | IC50 | = | 38.0 | nM | 7.42 |