Assay Detail
Functional
CHEMBL5583180
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Inhibition of cell viability in human UMUC14 cells harboring FGFR3 S249C mutant 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 | UMUC14 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 7.65 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545376 | ERDAFITINIB | 4.0 | 1 | 8.42 |
| CHEMBL5593800 | — | — | 1 | 8.00 |
| CHEMBL5595947 | — | — | 1 | 8.00 |
| CHEMBL5592211 | — | — | 1 | 7.89 |
| CHEMBL5590817 | — | — | 1 | 7.82 |
| CHEMBL5595500 | — | — | 1 | 7.80 |
| CHEMBL5584069 | — | — | 1 | 7.47 |
| CHEMBL5592556 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545376 | ERDAFITINIB | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5593800 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5595947 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5592211 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5590817 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5595500 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5584069 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5592556 | — | IC50 | = | 1578.0 | nM | 5.80 |