Assay Detail
Binding
CHEMBL5583159
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Inhibition of recombinant TEL/VEGFR2 (unknown origin) transduced in mouse BaF3 cells incubated for 48 hrs by Cell Titer Glo assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 7 — Homologous single protein target |
| 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 | 14 | 6.47 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | 1.0 | 1 | 8.05 |
| CHEMBL5593851 | — | — | 1 | 6.79 |
| CHEMBL5591286 | — | — | 1 | 6.70 |
| CHEMBL5591378 | — | — | 1 | 6.50 |
| CHEMBL5594702 | — | — | 1 | 6.49 |
| CHEMBL5595996 | — | — | 1 | 6.25 |
| CHEMBL5590027 | — | — | 1 | 6.23 |
| CHEMBL3545376 | ERDAFITINIB | 4.0 | 1 | 6.20 |
| CHEMBL5590821 | — | — | 1 | 6.20 |
| CHEMBL5594925 | — | — | 1 | 6.17 |
| CHEMBL5594374 | — | — | 1 | 6.06 |
| CHEMBL5594969 | — | — | 1 | 6.05 |
| CHEMBL5589661 | — | — | 1 | - |
| CHEMBL5595795 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5593851 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL5591286 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL5591378 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL5594702 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL5595996 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5590027 | — | IC50 | = | 586.0 | nM | 6.23 |
| CHEMBL3545376 | ERDAFITINIB | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL5590821 | — | IC50 | = | 637.0 | nM | 6.20 |
| CHEMBL5594925 | — | IC50 | = | 679.0 | nM | 6.17 |
| CHEMBL5594374 | — | IC50 | = | 864.0 | nM | 6.06 |
| CHEMBL5594969 | — | IC50 | = | 887.0 | nM | 6.05 |
| CHEMBL5589661 | — | IC50 | - | — | - | |
| CHEMBL5595795 | — | IC50 | - | — | - |