Assay Detail
Binding
CHEMBL4339035
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by TGFbeta-stimulation for 15 mins by array scan based method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Neovison vison |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.35 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4584495 | — | — | 1 | 6.70 |
| CHEMBL4514379 | — | — | 1 | 6.46 |
| CHEMBL4458215 | — | — | 1 | 6.38 |
| CHEMBL4455462 | — | — | 1 | 6.25 |
| CHEMBL4440988 | — | — | 1 | 6.18 |
| CHEMBL4452178 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4584495 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4514379 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4458215 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4455462 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4440988 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4452178 | — | IC50 | = | 800.0 | nM | 6.10 |