Assay Detail
Binding
CHEMBL4188412
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Inhibition of wild type His-tagged TGFbetaR2 (unknown origin) after 1 hr by HTRF assay
22
Total Activities
22
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 | 22 | 6.14 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205311 | — | — | 1 | 7.11 |
| CHEMBL4204772 | — | — | 1 | 6.96 |
| CHEMBL260015 | — | — | 1 | 6.72 |
| CHEMBL4210246 | — | — | 1 | 6.51 |
| CHEMBL4206793 | — | — | 1 | 6.26 |
| CHEMBL4205457 | — | — | 1 | 6.24 |
| CHEMBL4206220 | — | — | 1 | 6.09 |
| CHEMBL4209583 | — | — | 1 | 6.03 |
| CHEMBL4205979 | — | — | 1 | 5.96 |
| CHEMBL4209835 | — | — | 1 | 5.96 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 5.89 |
| CHEMBL4214470 | — | — | 1 | 5.70 |
| CHEMBL4217935 | — | — | 1 | 5.52 |
| CHEMBL4202469 | — | — | 1 | 5.07 |
| CHEMBL4210079 | — | — | 1 | - |
| CHEMBL4211574 | — | — | 1 | - |
| CHEMBL4216706 | — | — | 1 | - |
| CHEMBL4218893 | — | — | 1 | - |
| CHEMBL4206910 | — | — | 1 | - |
| CHEMBL4214237 | — | — | 1 | - |
| CHEMBL4205456 | — | — | 1 | - |
| CHEMBL4217699 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205311 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4204772 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL260015 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4210246 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4206793 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4205457 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4206220 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4209583 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4205979 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4209835 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2364611 | GALUNISERTIB | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4214470 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4217935 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4202469 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4210079 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4211574 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4216706 | — | IC50 | - | — | - | |
| CHEMBL4218893 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4206910 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4214237 | — | IC50 | - | — | - | |
| CHEMBL4205456 | — | IC50 | - | — | - | |
| CHEMBL4217699 | — | IC50 | > | 15000.0 | nM | - |