Assay Detail
Binding
CHEMBL1012778
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone by scintillation proximity assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.00 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218006 | — | — | 1 | 7.66 |
| CHEMBL458086 | — | — | 1 | 7.66 |
| CHEMBL517874 | — | — | 1 | 7.60 |
| CHEMBL456538 | — | — | 1 | 7.60 |
| CHEMBL512907 | — | — | 1 | 7.58 |
| CHEMBL458085 | — | — | 1 | 7.58 |
| CHEMBL510937 | — | — | 1 | 7.55 |
| CHEMBL459966 | — | — | 1 | 7.52 |
| CHEMBL456537 | — | — | 1 | 7.47 |
| CHEMBL455907 | — | — | 1 | 7.46 |
| CHEMBL516847 | — | — | 1 | 7.36 |
| CHEMBL518506 | — | — | 1 | 7.34 |
| CHEMBL460393 | — | — | 1 | 7.31 |
| CHEMBL517864 | — | — | 1 | 7.22 |
| CHEMBL461879 | — | — | 1 | 7.19 |
| CHEMBL455895 | — | — | 1 | 7.12 |
| CHEMBL517865 | — | — | 1 | 7.10 |
| CHEMBL516294 | — | — | 1 | 7.08 |
| CHEMBL505071 | — | — | 1 | 7.08 |
| CHEMBL456528 | — | — | 1 | 7.00 |
| CHEMBL512731 | — | — | 1 | 6.96 |
| CHEMBL509257 | — | — | 1 | 6.92 |
| CHEMBL506519 | — | — | 1 | 6.89 |
| CHEMBL464388 | — | — | 1 | 6.68 |
| CHEMBL456539 | — | — | 1 | 6.68 |
| CHEMBL455893 | — | — | 1 | 6.66 |
| CHEMBL459967 | — | — | 1 | 6.66 |
| CHEMBL455894 | — | — | 1 | 6.62 |
| CHEMBL461878 | — | — | 1 | 6.54 |
| CHEMBL464387 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218006 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL458086 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL517874 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL456538 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL512907 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL458085 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL510937 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL459966 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL456537 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL455907 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL516847 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL518506 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL460393 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL517864 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL461879 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL455895 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL517865 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL516294 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL505071 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL456528 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL512731 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL509257 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL506519 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL464388 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL456539 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL455893 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL459967 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL455894 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL461878 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL464387 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL517936 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL463775 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL509749 | — | Ki | = | 6500.0 | nM | 5.19 |