Assay Detail
Binding
CHEMBL1764081
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse 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 | Mus musculus |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL3910) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 8.32 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1761310 | — | — | 1 | 9.00 |
| CHEMBL1761137 | — | — | 1 | 8.89 |
| CHEMBL1761142 | — | — | 1 | 8.82 |
| CHEMBL1761320 | — | — | 1 | 8.82 |
| CHEMBL1761318 | — | — | 1 | 8.80 |
| CHEMBL1761136 | — | — | 1 | 8.77 |
| CHEMBL1760014 | — | — | 1 | 8.74 |
| CHEMBL1761323 | — | — | 1 | 8.74 |
| CHEMBL1761140 | — | — | 1 | 8.70 |
| CHEMBL1761141 | — | — | 1 | 8.70 |
| CHEMBL1761143 | — | — | 1 | 8.70 |
| CHEMBL1761319 | — | — | 1 | 8.66 |
| CHEMBL1761322 | MK-0736 | 2.0 | 1 | 8.62 |
| CHEMBL1761309 | — | — | 1 | 8.54 |
| CHEMBL383352 | — | — | 1 | 8.52 |
| CHEMBL1761327 | — | — | 1 | 8.52 |
| CHEMBL200513 | — | — | 1 | 8.52 |
| CHEMBL1761316 | — | — | 1 | 8.44 |
| CHEMBL1761311 | — | — | 1 | 8.41 |
| CHEMBL1761144 | — | — | 1 | 8.40 |
| CHEMBL1761321 | — | — | 1 | 8.40 |
| CHEMBL1761314 | — | — | 1 | 8.39 |
| CHEMBL1761317 | — | — | 1 | 8.20 |
| CHEMBL1761315 | — | — | 1 | 8.17 |
| CHEMBL1761313 | — | — | 1 | 8.01 |
| CHEMBL1761312 | — | — | 1 | 8.00 |
| CHEMBL1761324 | — | — | 1 | 7.96 |
| CHEMBL1761328 | — | — | 1 | 7.80 |
| CHEMBL1761135 | — | — | 1 | 7.72 |
| CHEMBL1761329 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1761310 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1761137 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1761142 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1761320 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1761318 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1761136 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1760014 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1761323 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1761140 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1761141 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1761143 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1761319 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1761322 | MK-0736 | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1761309 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL200513 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL383352 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1761327 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1761316 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1761311 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1761144 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1761321 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1761314 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1761317 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL1761315 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL1761313 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL1761312 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1761324 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1761328 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1761135 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1761329 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1761330 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1761325 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1761138 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL1761139 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL1761326 | — | IC50 | > | 4000.0 | nM | - |