Assay Detail
Binding
CHEMBL1018652
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Inhibition of full length human recombinant 11beta-HSD1 expressed in HEK293 cells in absence of NADPH
16
Total Activities
16
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
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.22 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL515717 | — | — | 1 | 7.58 |
| CHEMBL473347 | — | — | 1 | 7.57 |
| CHEMBL518644 | — | — | 1 | 7.44 |
| CHEMBL2021498 | — | — | 1 | 7.41 |
| CHEMBL2021497 | — | — | 1 | 7.39 |
| CHEMBL2021499 | — | — | 1 | 7.32 |
| CHEMBL460933 | — | — | 1 | 7.32 |
| CHEMBL526305 | — | — | 1 | 7.28 |
| CHEMBL517760 | — | — | 1 | 7.21 |
| CHEMBL460923 | — | — | 1 | 7.09 |
| CHEMBL2021500 | — | — | 1 | 7.02 |
| CHEMBL462154 | — | — | 1 | 7.01 |
| CHEMBL517434 | — | — | 1 | 6.77 |
| CHEMBL460924 | — | — | 1 | 6.72 |
| CHEMBL516674 | — | — | 1 | - |
| CHEMBL463225 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL515717 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL473347 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL518644 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2021498 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2021497 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2021499 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL460933 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL526305 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL517760 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL460923 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2021500 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL462154 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL517434 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL460924 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL516674 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL463225 | — | IC50 | > | 300.0 | nM | - |