Assay Detail
Binding
CHEMBL1018653
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Inhibition of FLAG-tagged full length human 11beta-HSD1 expressed in baculovirus-infected Trichoplusia ni Hi5 cells assessed as reduction of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BTI-TN-5B1-4 |
| 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 | 23 | 8.11 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511828 | — | — | 1 | 9.12 |
| CHEMBL469699 | — | — | 1 | 8.89 |
| CHEMBL518644 | — | — | 1 | 8.82 |
| CHEMBL455443 | — | — | 1 | 8.80 |
| CHEMBL2021495 | — | — | 1 | 8.80 |
| CHEMBL2021496 | — | — | 1 | 8.80 |
| CHEMBL452587 | — | — | 1 | 8.77 |
| CHEMBL517760 | — | — | 1 | 8.77 |
| CHEMBL2021499 | — | — | 1 | 8.48 |
| CHEMBL473347 | — | — | 1 | 8.38 |
| CHEMBL463031 | — | — | 1 | 8.31 |
| CHEMBL515717 | — | — | 1 | 8.24 |
| CHEMBL460933 | — | — | 1 | 8.05 |
| CHEMBL2021500 | — | — | 1 | 7.96 |
| CHEMBL526305 | — | — | 1 | 7.85 |
| CHEMBL2021497 | — | — | 1 | 7.77 |
| CHEMBL2021498 | — | — | 1 | 7.66 |
| CHEMBL462154 | — | — | 1 | 7.58 |
| CHEMBL517434 | — | — | 1 | 7.47 |
| CHEMBL460923 | — | — | 1 | 7.37 |
| CHEMBL460924 | — | — | 1 | 7.19 |
| CHEMBL516674 | — | — | 1 | 6.82 |
| CHEMBL463225 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511828 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL469699 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL518644 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL455443 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2021495 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2021496 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL452587 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL517760 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2021499 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL473347 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL463031 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL515717 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL460933 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2021500 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL526305 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2021497 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2021498 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL462154 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL517434 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL460923 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL460924 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL516674 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL463225 | — | IC50 | = | 190.0 | nM | 6.72 |