Assay Detail
Binding
CHEMBL1013588
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 11beta-HSD1 expressed in CHO cells assessed as conversion of cortisone to cortisol by ELISA
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| IC50 | 22 | 7.30 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL373257 | — | — | 1 | 8.66 |
| CHEMBL375156 | — | — | 1 | 8.30 |
| CHEMBL462305 | — | — | 1 | 8.30 |
| CHEMBL517874 | — | — | 1 | 7.96 |
| CHEMBL462304 | — | — | 1 | 7.85 |
| CHEMBL512907 | — | — | 1 | 7.75 |
| CHEMBL460393 | — | — | 1 | 7.50 |
| CHEMBL455907 | — | — | 1 | 7.47 |
| CHEMBL456538 | — | — | 1 | 7.37 |
| CHEMBL461879 | — | — | 1 | 7.29 |
| CHEMBL458086 | — | — | 1 | 7.28 |
| CHEMBL456537 | — | — | 1 | 7.16 |
| CHEMBL512731 | — | — | 1 | 7.11 |
| CHEMBL516847 | — | — | 1 | 7.10 |
| CHEMBL518506 | — | — | 1 | 6.96 |
| CHEMBL459966 | — | — | 1 | 6.96 |
| CHEMBL517865 | — | — | 1 | 6.89 |
| CHEMBL455893 | — | — | 1 | 6.75 |
| CHEMBL383146 | — | — | 1 | 6.72 |
| CHEMBL456539 | — | — | 1 | 6.52 |
| CHEMBL461878 | — | — | 1 | 6.51 |
| CHEMBL517864 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL373257 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL375156 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL462305 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL517874 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL462304 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL512907 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL460393 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL455907 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL456538 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL461879 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL458086 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL456537 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL512731 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL516847 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL518506 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL459966 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL517865 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL455893 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL383146 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL456539 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL461878 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL517864 | — | IC50 | = | 680.0 | nM | 6.17 |