Assay Detail
Binding
CHEMBL1646345
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat 11beta-HSD1 assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
4
Total Activities
4
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 |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL2391) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.02 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1642603 | — | — | 1 | 7.52 |
| CHEMBL1642595 | — | — | 1 | 7.07 |
| CHEMBL1642600 | — | — | 1 | 6.84 |
| CHEMBL1642602 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1642603 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1642595 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1642600 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL1642602 | — | IC50 | = | 220.0 | nM | 6.66 |