Assay Detail
Binding
CHEMBL4339037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysis
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
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 | 7 | 8.68 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4455462 | — | — | 1 | 9.15 |
| CHEMBL4440988 | — | — | 1 | 9.05 |
| CHEMBL4458215 | — | — | 1 | 9.00 |
| CHEMBL4584495 | — | — | 1 | 8.80 |
| CHEMBL4514379 | — | — | 1 | 8.80 |
| CHEMBL4452178 | — | — | 1 | 8.17 |
| CHEMBL4534989 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4455462 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4440988 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4458215 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4584495 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4514379 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4452178 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4534989 | — | IC50 | = | 17.0 | nM | 7.77 |