Assay Detail
Functional
CHEMBL829583
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Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.88 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365663 | GW780159X | — | 1 | 8.00 |
| CHEMBL185238 | GW786460X | — | 1 | 8.00 |
| CHEMBL360034 | — | — | 1 | 8.00 |
| CHEMBL361237 | GW785804X | — | 1 | 7.52 |
| CHEMBL183354 | — | — | 1 | 7.30 |
| CHEMBL181361 | GW693481X | — | 1 | 6.92 |
| CHEMBL182354 | — | — | 1 | 6.66 |
| CHEMBL425177 | — | — | 1 | 6.58 |
| CHEMBL181640 | — | — | 1 | 6.38 |
| CHEMBL362710 | — | — | 1 | 5.18 |
| CHEMBL184746 | — | — | 1 | 5.18 |
| CHEMBL359724 | — | — | 1 | - |
| CHEMBL185237 | — | — | 1 | - |
| CHEMBL186966 | — | — | 1 | - |
| CHEMBL365918 | — | — | 1 | - |
| CHEMBL447486 | — | — | 1 | - |
| CHEMBL360613 | — | — | 1 | - |
| CHEMBL181958 | — | — | 1 | - |
| CHEMBL359611 | — | — | 1 | - |
| CHEMBL182678 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365663 | GW780159X | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL185238 | GW786460X | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL360034 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL361237 | GW785804X | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL183354 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL181361 | GW693481X | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL182354 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL425177 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL181640 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL362710 | — | IC50 | = | 6580.0 | nM | 5.18 |
| CHEMBL184746 | — | IC50 | = | 6670.0 | nM | 5.18 |
| CHEMBL359724 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL185237 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL186966 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL365918 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL447486 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL360613 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL181958 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL359611 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL182678 | — | IC50 | > | 10000.0 | nM | - |