Assay Detail
Binding
CHEMBL1646336
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Inhibition of human recombinant full length 11beta-HSD1 expressed in human adipocytes assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of 3% human serum albumin
14
Total Activities
14
Compounds Tested
1
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
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.70 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1642595 | — | — | 1 | 8.06 |
| CHEMBL1642601 | — | — | 1 | 7.92 |
| CHEMBL1642600 | — | — | 1 | 7.85 |
| CHEMBL1642589 | — | — | 1 | 7.82 |
| CHEMBL1642593 | — | — | 1 | 7.77 |
| CHEMBL1642596 | — | — | 1 | 7.77 |
| CHEMBL1642603 | — | — | 1 | 7.75 |
| CHEMBL1642594 | — | — | 1 | 7.70 |
| CHEMBL1642598 | — | — | 1 | 7.62 |
| CHEMBL1642602 | — | — | 1 | 7.60 |
| CHEMBL1642587 | — | — | 1 | 7.51 |
| CHEMBL1642597 | — | — | 1 | 7.44 |
| CHEMBL526305 | — | — | 1 | 7.30 |
| CHEMBL1642599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1642595 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL1642601 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1642600 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1642589 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1642593 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1642596 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1642603 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1642594 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1642598 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1642602 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1642587 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1642597 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL526305 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1642599 | — | IC50 | > | 100.0 | nM | - |