Assay Detail
Binding
CHEMBL861562
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Inhibition of recombinant human TGFbeta R1 expressed in Sf9 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.54 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204966 | — | — | 1 | 7.66 |
| CHEMBL204063 | — | — | 1 | 7.39 |
| CHEMBL382838 | — | — | 1 | 7.33 |
| CHEMBL261454 | — | — | 1 | 7.23 |
| CHEMBL381532 | — | — | 1 | 7.16 |
| CHEMBL206233 | — | — | 1 | 7.13 |
| CHEMBL204170 | — | — | 1 | 7.12 |
| CHEMBL203619 | — | — | 1 | 7.10 |
| CHEMBL441176 | — | — | 1 | 7.07 |
| CHEMBL203791 | — | — | 1 | 6.91 |
| CHEMBL377711 | — | — | 1 | 6.81 |
| CHEMBL378167 | — | — | 1 | 6.61 |
| CHEMBL202730 | — | — | 1 | 6.40 |
| CHEMBL204139 | — | — | 1 | 5.77 |
| CHEMBL202625 | — | — | 1 | 5.74 |
| CHEMBL377717 | — | — | 1 | 5.39 |
| CHEMBL203214 | — | — | 1 | 5.32 |
| CHEMBL204158 | — | — | 1 | 5.18 |
| CHEMBL427211 | — | — | 1 | 4.91 |
| CHEMBL204061 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204966 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL204063 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL382838 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL261454 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL381532 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL206233 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL204170 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL203619 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL441176 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL203791 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL377711 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL378167 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL202730 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL204139 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL202625 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL377717 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL203214 | — | IC50 | = | 4740.0 | nM | 5.32 |
| CHEMBL204158 | — | IC50 | = | 6580.0 | nM | 5.18 |
| CHEMBL427211 | — | IC50 | = | 12230.0 | nM | 4.91 |
| CHEMBL204061 | — | IC50 | > | 20000.0 | nM | - |