Assay Detail
Binding
CHEMBL928261
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Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.60 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL409525 | — | — | 1 | 7.62 |
| CHEMBL261762 | — | — | 1 | 7.48 |
| CHEMBL411855 | — | — | 1 | 7.33 |
| CHEMBL409356 | — | — | 1 | 7.31 |
| CHEMBL261454 | — | — | 1 | 7.23 |
| CHEMBL260015 | — | — | 1 | 7.16 |
| CHEMBL406411 | — | — | 1 | 7.14 |
| CHEMBL261674 | — | — | 1 | 7.13 |
| CHEMBL411297 | — | — | 1 | 7.07 |
| CHEMBL260923 | — | — | 1 | 7.05 |
| CHEMBL409331 | — | — | 1 | 7.00 |
| CHEMBL409158 | — | — | 1 | 6.89 |
| CHEMBL260240 | — | — | 1 | 6.85 |
| CHEMBL260147 | — | — | 1 | 6.80 |
| CHEMBL410308 | — | — | 1 | 6.71 |
| CHEMBL408181 | — | — | 1 | 6.28 |
| CHEMBL260239 | — | — | 1 | 6.12 |
| CHEMBL411741 | — | — | 1 | 6.03 |
| CHEMBL261702 | — | — | 1 | 5.96 |
| CHEMBL260729 | — | — | 1 | 5.96 |
| CHEMBL258641 | — | — | 1 | 5.92 |
| CHEMBL261625 | — | — | 1 | 5.42 |
| CHEMBL261701 | — | — | 1 | 5.32 |
| CHEMBL406407 | — | — | 1 | 4.70 |
| CHEMBL409515 | — | — | 1 | - |
| CHEMBL259169 | — | — | 1 | - |
| CHEMBL258964 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL409525 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL261762 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL411855 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL409356 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL261454 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL260015 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL406411 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL261674 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL411297 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL260923 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL409331 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL409158 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL260240 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL260147 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL410308 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL408181 | — | IC50 | = | 526.0 | nM | 6.28 |
| CHEMBL260239 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL411741 | — | IC50 | = | 928.0 | nM | 6.03 |
| CHEMBL261702 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL260729 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL258641 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL261625 | — | IC50 | = | 3810.0 | nM | 5.42 |
| CHEMBL261701 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL406407 | — | IC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL409515 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL259169 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL258964 | — | IC50 | > | 20000.0 | nM | - |