Assay Detail
Binding
CHEMBL4361670
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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 radiometric assay
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
Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.10 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3260567 | VACTOSERTIB | 2.0 | 1 | 8.00 |
| CHEMBL4569982 | — | — | 1 | 7.52 |
| CHEMBL4527908 | — | — | 1 | 7.52 |
| CHEMBL4576703 | — | — | 1 | 7.41 |
| CHEMBL4594036 | — | — | 1 | 7.38 |
| CHEMBL4461256 | — | — | 1 | 7.26 |
| CHEMBL4513885 | — | — | 1 | 7.11 |
| CHEMBL4471215 | — | — | 1 | 7.06 |
| CHEMBL4455044 | — | — | 1 | 6.94 |
| CHEMBL4520187 | — | — | 1 | 6.92 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 6.92 |
| CHEMBL4570292 | — | — | 1 | 6.90 |
| CHEMBL4530888 | — | — | 1 | 6.78 |
| CHEMBL4474331 | — | — | 1 | 6.78 |
| CHEMBL4531718 | — | — | 1 | 6.64 |
| CHEMBL4460586 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3260567 | VACTOSERTIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4569982 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4527908 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4576703 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4594036 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4461256 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4513885 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4471215 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4455044 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4520187 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL2364611 | GALUNISERTIB | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL4570292 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4530888 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4474331 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4531718 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4460586 | — | IC50 | = | 312.0 | nM | 6.51 |