Assay Detail
Binding
CHEMBL1827133
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Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sterol regulatory element-binding protein 2 (CHEMBL1795166) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.26 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL169046 | — | — | 1 | 6.52 |
| CHEMBL1824673 | — | — | 1 | 6.16 |
| CHEMBL1824674 | — | — | 1 | 6.05 |
| CHEMBL1824676 | — | — | 1 | 5.72 |
| CHEMBL1824675 | — | — | 1 | 5.64 |
| CHEMBL1824669 | — | — | 1 | 5.55 |
| CHEMBL1824670 | — | — | 1 | 5.52 |
| CHEMBL1824664 | — | — | 1 | 5.50 |
| CHEMBL1824671 | — | — | 1 | 5.31 |
| CHEMBL1621019 | FATOSTATIN | — | 1 | 5.25 |
| CHEMBL1824658 | — | — | 1 | 5.17 |
| CHEMBL1824672 | — | — | 1 | 5.15 |
| CHEMBL1824661 | — | — | 1 | 5.11 |
| CHEMBL1824668 | — | — | 1 | 5.07 |
| CHEMBL1824665 | — | — | 1 | 5.02 |
| CHEMBL1824666 | — | — | 1 | 5.02 |
| CHEMBL1616869 | — | — | 1 | 5.01 |
| CHEMBL1824663 | — | — | 1 | 4.99 |
| CHEMBL1622565 | — | — | 1 | 4.97 |
| CHEMBL1824660 | — | — | 1 | 4.91 |
| CHEMBL1824662 | — | — | 1 | 4.89 |
| CHEMBL1824667 | — | — | 1 | 4.84 |
| CHEMBL1824655 | — | — | 1 | 4.83 |
| CHEMBL1824656 | — | — | 1 | 4.73 |
| CHEMBL1824659 | — | — | 1 | 4.64 |
| CHEMBL1300882 | — | — | 1 | - |
| CHEMBL1824657 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL169046 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1824673 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1824674 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1824676 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1824675 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1824669 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1824670 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1824664 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1824671 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1621019 | FATOSTATIN | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1824658 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL1824672 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL1824661 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL1824668 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL1824665 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL1824666 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL1616869 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1824663 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL1622565 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL1824660 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL1824662 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1824667 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL1824655 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL1824656 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL1824659 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL1300882 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1824657 | — | IC50 | > | 30000.0 | nM | - |