Assay Detail
Functional
CHEMBL860754
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Inhibition of TGF beta-induced transcription of firefly luciferase reporter gene in HepG2 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.60 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424676 | — | — | 1 | 7.85 |
| CHEMBL202994 | — | — | 1 | 7.30 |
| CHEMBL202887 | — | — | 1 | 7.03 |
| CHEMBL204211 | — | — | 1 | 6.98 |
| CHEMBL205570 | — | — | 1 | 6.93 |
| CHEMBL208437 | GW711782X | — | 1 | 6.88 |
| CHEMBL205158 | GW695874X | — | 1 | 6.68 |
| CHEMBL436944 | — | — | 1 | 6.59 |
| CHEMBL202943 | — | — | 1 | 6.57 |
| CHEMBL1237161 | — | — | 1 | 6.45 |
| CHEMBL206017 | — | — | 1 | 6.31 |
| CHEMBL205736 | — | — | 1 | 6.29 |
| CHEMBL379700 | — | — | 1 | 6.28 |
| CHEMBL205151 | — | — | 1 | 6.27 |
| CHEMBL380916 | — | — | 1 | 6.27 |
| CHEMBL202891 | GW679410X | — | 1 | 6.27 |
| CHEMBL204575 | — | — | 1 | 6.16 |
| CHEMBL205271 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424676 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL202994 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL202887 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL204211 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL205570 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL208437 | GW711782X | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL205158 | GW695874X | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL436944 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL202943 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL1237161 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL206017 | — | IC50 | = | 486.0 | nM | 6.31 |
| CHEMBL205736 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL379700 | — | IC50 | = | 529.0 | nM | 6.28 |
| CHEMBL205151 | — | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL380916 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL202891 | GW679410X | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL204575 | — | IC50 | = | 693.0 | nM | 6.16 |
| CHEMBL205271 | — | IC50 | = | 1691.0 | nM | 5.77 |