Assay Detail
Binding
CHEMBL1764083
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]-cortisone to [3H]-cortisol by scintillation proximity assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.09 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1761143 | — | — | 1 | 9.00 |
| CHEMBL1761142 | — | — | 1 | 8.96 |
| CHEMBL1761137 | — | — | 1 | 8.92 |
| CHEMBL1761323 | — | — | 1 | 8.80 |
| CHEMBL383352 | — | — | 1 | 8.74 |
| CHEMBL1761140 | — | — | 1 | 8.70 |
| CHEMBL1761327 | — | — | 1 | 8.55 |
| CHEMBL1761322 | MK-0736 | 2.0 | 1 | 8.49 |
| CHEMBL1761311 | — | — | 1 | 8.48 |
| CHEMBL1761320 | — | — | 1 | 8.43 |
| CHEMBL200513 | — | — | 1 | 8.40 |
| CHEMBL1761141 | — | — | 1 | 8.40 |
| CHEMBL1761312 | — | — | 1 | 8.39 |
| CHEMBL1761316 | — | — | 1 | 8.39 |
| CHEMBL1761318 | — | — | 1 | 8.36 |
| CHEMBL1761315 | — | — | 1 | 8.29 |
| CHEMBL1761317 | — | — | 1 | 8.27 |
| CHEMBL1760014 | — | — | 1 | 8.26 |
| CHEMBL1761319 | — | — | 1 | 8.21 |
| CHEMBL1761313 | — | — | 1 | 8.15 |
| CHEMBL1761324 | — | — | 1 | 8.12 |
| CHEMBL1761310 | — | — | 1 | 8.09 |
| CHEMBL1761328 | — | — | 1 | 8.00 |
| CHEMBL1761314 | — | — | 1 | 7.96 |
| CHEMBL1761309 | — | — | 1 | 7.70 |
| CHEMBL1761329 | — | — | 1 | 7.70 |
| CHEMBL1761321 | — | — | 1 | 7.60 |
| CHEMBL1761144 | — | — | 1 | 7.52 |
| CHEMBL1761135 | — | — | 1 | 7.46 |
| CHEMBL1761330 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1761143 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1761142 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1761137 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1761323 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL383352 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1761140 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1761327 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL1761322 | MK-0736 | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1761311 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1761320 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL200513 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1761141 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1761312 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1761316 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1761318 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1761315 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1761317 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1760014 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL1761319 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL1761313 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1761324 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL1761310 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL1761328 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1761314 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1761309 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1761329 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1761321 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1761144 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1761135 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1761330 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1761325 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1761326 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1761136 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL1761138 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL1761139 | — | IC50 | < | 1.0 | nM | - |