Assay Detail
Binding
CHEMBL1646335
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full length 11beta-HSD1 expressed in HEK293 cells assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of 3% human serum albumin
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 14 | 7.14 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1642595 | — | — | 1 | 7.70 |
| CHEMBL1642601 | — | — | 1 | 7.47 |
| CHEMBL1642589 | — | — | 1 | 7.46 |
| CHEMBL1642593 | — | — | 1 | 7.43 |
| CHEMBL1642598 | — | — | 1 | 7.26 |
| CHEMBL1642603 | — | — | 1 | 7.20 |
| CHEMBL1642602 | — | — | 1 | 7.13 |
| CHEMBL1642592 | — | — | 1 | 7.04 |
| CHEMBL1642587 | — | — | 1 | 7.03 |
| CHEMBL1642597 | — | — | 1 | 6.96 |
| CHEMBL526305 | — | — | 1 | 6.92 |
| CHEMBL1642596 | — | — | 1 | 6.89 |
| CHEMBL1642600 | — | — | 1 | 6.87 |
| CHEMBL1642594 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1642595 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1642601 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1642589 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1642593 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1642598 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1642603 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1642602 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1642592 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL1642587 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL1642597 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL526305 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL1642596 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1642600 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1642594 | — | IC50 | = | 259.0 | nM | 6.59 |