Assay Detail
Binding
CHEMBL4188417
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TGFbetaR1 in human primary T-cells assessed as TGFbeta-stimulated PSMAD phosphorylation preincubated for 1 hr followed by TGFbeta addition measured after 90 mins by Alpha screen assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.41 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210246 | — | — | 1 | 8.29 |
| CHEMBL4209583 | — | — | 1 | 7.92 |
| CHEMBL4209835 | — | — | 1 | 7.58 |
| CHEMBL4205456 | — | — | 1 | 7.30 |
| CHEMBL4216706 | — | — | 1 | 6.92 |
| CHEMBL260015 | — | — | 1 | 6.43 |
| CHEMBL4217699 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210246 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4209583 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4209835 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4205456 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4216706 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL260015 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4217699 | — | IC50 | - | — | - |