Assay Detail
Binding
CHEMBL5234111
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Inhibition of TbetaR-1 (unknown origin)
8
Total Activities
8
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
Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.64 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4303194 | — | — | 1 | 8.60 |
| CHEMBL1170377 | — | — | 1 | 7.92 |
| CHEMBL202887 | — | — | 1 | 7.75 |
| CHEMBL185238 | GW786460X | — | 1 | 7.64 |
| CHEMBL129677 | — | — | 1 | 7.60 |
| CHEMBL238125 | — | — | 1 | 7.32 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 7.25 |
| CHEMBL440084 | SB-431542 | — | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4303194 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1170377 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL202887 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL185238 | GW786460X | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL129677 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL238125 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2364611 | GALUNISERTIB | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL440084 | SB-431542 | IC50 | = | 94.0 | nM | 7.03 |