Assay Detail
Binding
CHEMBL1105684
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Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay
21
Total Activities
21
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
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 9.00 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1098145 | — | — | 1 | 10.52 |
| CHEMBL1096870 | — | — | 1 | 10.52 |
| CHEMBL1098130 | — | — | 1 | 10.52 |
| CHEMBL1098131 | — | — | 1 | 10.52 |
| CHEMBL1096451 | — | — | 1 | 10.52 |
| CHEMBL1097177 | — | — | 1 | 9.49 |
| CHEMBL1098159 | — | — | 1 | 9.49 |
| CHEMBL1097828 | — | — | 1 | 9.49 |
| CHEMBL1097827 | — | — | 1 | 9.49 |
| CHEMBL1097178 | — | — | 1 | 9.49 |
| CHEMBL1095787 | — | — | 1 | 9.47 |
| CHEMBL1088117 | — | — | 1 | 8.92 |
| CHEMBL1088115 | — | — | 1 | 8.66 |
| CHEMBL1095033 | — | — | 1 | 8.46 |
| CHEMBL1095047 | — | — | 1 | 8.38 |
| CHEMBL1095785 | — | — | 1 | 8.30 |
| CHEMBL1095786 | — | — | 1 | 8.00 |
| CHEMBL1098160 | — | — | 1 | 7.70 |
| CHEMBL1088116 | — | — | 1 | 7.66 |
| CHEMBL1088379 | — | — | 1 | 6.76 |
| CHEMBL1088517 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1098145 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL1096870 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL1098130 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL1098131 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL1096451 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL1097177 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1098159 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1097828 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1097827 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1097178 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1095787 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL1088117 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1088115 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1095033 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1095047 | — | IC50 | = | 4.15 | nM | 8.38 |
| CHEMBL1095785 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1095786 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1098160 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1088116 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1088379 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL1088517 | — | IC50 | = | 290.0 | nM | 6.54 |