Assay Detail
Binding
CHEMBL1105681
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Inhibition of human 11-beta-HSD1
21
Total Activities
21
Compounds Tested
2
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
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.60 | 9.00 |
| Ki(app) | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1095785 | — | — | 1 | 9.00 |
| CHEMBL1098159 | — | — | 1 | 9.00 |
| CHEMBL1097178 | — | — | 1 | 9.00 |
| CHEMBL1097827 | — | — | 1 | 9.00 |
| CHEMBL1095786 | — | — | 1 | 9.00 |
| CHEMBL1095047 | — | — | 1 | 8.85 |
| CHEMBL1088117 | — | — | 1 | 8.85 |
| CHEMBL1095033 | — | — | 1 | 8.80 |
| CHEMBL1097828 | — | — | 1 | 8.70 |
| CHEMBL1097177 | — | — | 1 | 8.62 |
| CHEMBL1088116 | — | — | 1 | 8.62 |
| CHEMBL1088115 | — | — | 1 | 8.51 |
| CHEMBL1098160 | — | — | 1 | 8.44 |
| CHEMBL1088517 | — | — | 1 | 7.82 |
| CHEMBL1088379 | — | — | 1 | 6.76 |
| CHEMBL1098145 | — | — | 1 | - |
| CHEMBL1098131 | — | — | 1 | - |
| CHEMBL1098130 | — | — | 1 | - |
| CHEMBL1096870 | — | — | 1 | - |
| CHEMBL1095787 | — | — | 1 | - |
| CHEMBL1096451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1095785 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1098159 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1097178 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1097827 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1095786 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1095047 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1088117 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1095033 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1097828 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1097177 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1088116 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1088115 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL1098160 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1088517 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1088379 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL1098145 | — | Ki(app) | - | — | - | |
| CHEMBL1098131 | — | Ki(app) | - | — | - | |
| CHEMBL1098130 | — | Ki(app) | - | — | - | |
| CHEMBL1096870 | — | Ki(app) | - | — | - | |
| CHEMBL1095787 | — | Ki(app) | - | — | - | |
| CHEMBL1096451 | — | Ki(app) | - | — | - |