Assay Detail
Binding
CHEMBL4339025
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Inhibition of wild type His-tagged TGFBR2 kinase domain (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 | 5.44 | 6.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4455462 | — | — | 1 | 6.09 |
| CHEMBL4440988 | — | — | 1 | 5.53 |
| CHEMBL4534989 | — | — | 1 | 5.24 |
| CHEMBL4458215 | — | — | 1 | 4.89 |
| CHEMBL4584495 | — | — | 1 | - |
| CHEMBL4452178 | — | — | 1 | - |
| CHEMBL4514379 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4455462 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4440988 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL4534989 | — | IC50 | = | 5710.0 | nM | 5.24 |
| CHEMBL4458215 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL4584495 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4452178 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4514379 | — | IC50 | > | 15000.0 | nM | - |