Assay Detail
Binding
CHEMBL4188416
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Inhibition of TGFbetaR1 in mink Mv1Lu cells assessed as TGFbeta-stimulated PSMAD2 phosphorylation preincubated for 1 hr followed by TGFbeta addition measured after 15 mins
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Neovison vison |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.64 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210246 | — | — | 1 | 7.62 |
| CHEMBL4209583 | — | — | 1 | 7.37 |
| CHEMBL4217699 | — | — | 1 | 7.33 |
| CHEMBL4214470 | — | — | 1 | 7.12 |
| CHEMBL4206793 | — | — | 1 | 7.00 |
| CHEMBL4205456 | — | — | 1 | 6.89 |
| CHEMBL4209835 | — | — | 1 | 6.82 |
| CHEMBL4216706 | — | — | 1 | 6.75 |
| CHEMBL4205457 | — | — | 1 | 6.75 |
| CHEMBL4214237 | — | — | 1 | 6.66 |
| CHEMBL4217935 | — | — | 1 | 6.51 |
| CHEMBL4205311 | — | — | 1 | 6.46 |
| CHEMBL4206220 | — | — | 1 | 6.41 |
| CHEMBL4204772 | — | — | 1 | 6.30 |
| CHEMBL4202469 | — | — | 1 | 6.15 |
| CHEMBL260015 | — | — | 1 | 6.12 |
| CHEMBL4211574 | — | — | 1 | 5.92 |
| CHEMBL4218893 | — | — | 1 | 5.41 |
| CHEMBL4206910 | — | — | 1 | - |
| CHEMBL4210079 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210246 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4209583 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4217699 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4214470 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4206793 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4205456 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4209835 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4216706 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4205457 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4214237 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4217935 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4205311 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4206220 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4204772 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4202469 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL260015 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4211574 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4218893 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4206910 | — | IC50 | - | — | - | |
| CHEMBL4210079 | — | IC50 | > | 10000.0 | nM | - |