Assay Detail
Binding
CHEMBL2154125
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Inhibition of SCD-1 activity in Sprague-Dawley rat microsome assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.88 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL594902 | — | — | 1 | 8.70 |
| CHEMBL1938870 | MK-8245 | 1.0 | 1 | 8.52 |
| CHEMBL2153601 | — | — | 1 | 8.15 |
| CHEMBL2153600 | — | — | 1 | 7.47 |
| CHEMBL2153599 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL594902 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1938870 | MK-8245 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2153601 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2153600 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2153599 | — | IC50 | = | 276.0 | nM | 6.56 |