Assay Detail
Binding
CHEMBL1014489
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Inhibition of human recombinant 11beta-HSD1 expressed HEK293 cells by scintillation proximity assay in presence of human serum albumin
15
Total Activities
15
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
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.99 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512355 | — | — | 1 | 7.96 |
| CHEMBL491326 | — | — | 1 | 7.55 |
| CHEMBL508331 | — | — | 1 | 7.52 |
| CHEMBL2021494 | — | — | 1 | 7.22 |
| CHEMBL2021502 | — | — | 1 | 7.11 |
| CHEMBL454620 | — | — | 1 | 7.05 |
| CHEMBL507804 | — | — | 1 | 7.01 |
| CHEMBL454621 | — | — | 1 | 6.97 |
| CHEMBL452587 | — | — | 1 | 6.91 |
| CHEMBL489320 | — | — | 1 | 6.89 |
| CHEMBL523600 | — | — | 1 | 6.89 |
| CHEMBL453620 | — | — | 1 | 6.83 |
| CHEMBL2021501 | — | — | 1 | 6.70 |
| CHEMBL2021493 | — | — | 1 | 6.38 |
| CHEMBL491327 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512355 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL491326 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL508331 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2021494 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2021502 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL454620 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL507804 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL454621 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL452587 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL489320 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL523600 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL453620 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL2021501 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL2021493 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL491327 | — | IC50 | = | 1190.0 | nM | 5.92 |