Assay Detail
Binding
CHEMBL1831613
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Inhibition of TGF-beta1 signaling in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.27 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1829511 | — | — | 1 | 7.96 |
| CHEMBL424676 | — | — | 1 | 7.72 |
| CHEMBL1829512 | — | — | 1 | 7.50 |
| CHEMBL1828640 | — | — | 1 | 7.17 |
| CHEMBL1829504 | — | — | 1 | 7.11 |
| CHEMBL1829505 | — | — | 1 | 7.06 |
| CHEMBL202887 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1829511 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL424676 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1829512 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1828640 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1829504 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1829505 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL202887 | — | IC50 | = | 446.0 | nM | 6.35 |