Assay Detail
Binding
CHEMBL3270799
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | 4T1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.47 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3260567 | VACTOSERTIB | 2.0 | 1 | 7.92 |
| CHEMBL492634 | — | — | 1 | 7.36 |
| CHEMBL226838 | — | — | 1 | 7.12 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3260567 | VACTOSERTIB | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL492634 | — | IC50 | = | 44.2 | nM | 7.36 |
| CHEMBL226838 | — | IC50 | = | 76.6 | nM | 7.12 |
| CHEMBL2364611 | GALUNISERTIB | IC50 | > | 100.0 | nM | - |