Assay Detail
Binding
CHEMBL4739183
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Inhibition of recombinant human GST-fused ALK5 expressed in baculovirus infected Sf9 cells assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method
16
Total Activities
16
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 | Autocuration |
Publication
Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.94 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748823 | — | — | 1 | 8.40 |
| CHEMBL4778963 | — | — | 1 | 8.40 |
| CHEMBL4779584 | — | — | 1 | 8.30 |
| CHEMBL4747557 | — | — | 1 | 8.30 |
| CHEMBL4780141 | — | — | 1 | 8.22 |
| CHEMBL4759911 | — | — | 1 | 8.10 |
| CHEMBL4798879 | — | — | 1 | 8.05 |
| CHEMBL4788508 | — | — | 1 | 8.00 |
| CHEMBL4794179 | — | — | 1 | 7.96 |
| CHEMBL4752915 | — | — | 1 | 7.89 |
| CHEMBL4756404 | — | — | 1 | 7.85 |
| CHEMBL3260567 | VACTOSERTIB | 2.0 | 1 | 7.85 |
| CHEMBL4784124 | — | — | 1 | 7.80 |
| CHEMBL4780013 | — | — | 1 | 7.62 |
| CHEMBL4740767 | — | — | 1 | 7.47 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748823 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4778963 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4779584 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4747557 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4780141 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4759911 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4798879 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4788508 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4794179 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4752915 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4756404 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3260567 | VACTOSERTIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4784124 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4780013 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4740767 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2364611 | GALUNISERTIB | IC50 | = | 129.0 | nM | 6.89 |