Assay Detail
Binding
CHEMBL4434540
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Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting 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 biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.70 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4519261 | — | — | 1 | 8.10 |
| CHEMBL4588407 | — | — | 1 | 8.00 |
| CHEMBL4453060 | — | — | 1 | 7.96 |
| CHEMBL4574187 | — | — | 1 | 7.89 |
| CHEMBL4464656 | — | — | 1 | 7.85 |
| CHEMBL4474911 | — | — | 1 | 7.85 |
| CHEMBL3260567 | VACTOSERTIB | 2.0 | 1 | 7.85 |
| CHEMBL4576341 | — | — | 1 | 7.77 |
| CHEMBL4543738 | — | — | 1 | 7.72 |
| CHEMBL4534375 | — | — | 1 | 7.68 |
| CHEMBL4553389 | — | — | 1 | 7.66 |
| CHEMBL4516224 | — | — | 1 | 7.64 |
| CHEMBL4447399 | — | — | 1 | 7.60 |
| CHEMBL4533727 | — | — | 1 | 7.38 |
| CHEMBL4519255 | — | — | 1 | 7.37 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4519261 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4588407 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4453060 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4574187 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4464656 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4474911 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3260567 | VACTOSERTIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4576341 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4543738 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4534375 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4553389 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4516224 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4447399 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4533727 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4519255 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2364611 | GALUNISERTIB | IC50 | = | 129.0 | nM | 6.89 |