Assay Detail
Binding
CHEMBL1014487
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Inhibition of human recombinant 11beta-HSD1 expressed in baculovirus system by scintillation proximity assay
15
Total Activities
15
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
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 | 8.46 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491326 | — | — | 1 | 9.22 |
| CHEMBL512355 | — | — | 1 | 9.15 |
| CHEMBL508331 | — | — | 1 | 9.06 |
| CHEMBL452587 | — | — | 1 | 8.85 |
| CHEMBL454620 | — | — | 1 | 8.77 |
| CHEMBL523600 | — | — | 1 | 8.70 |
| CHEMBL2021502 | — | — | 1 | 8.62 |
| CHEMBL489320 | — | — | 1 | 8.55 |
| CHEMBL507804 | — | — | 1 | 8.42 |
| CHEMBL2021494 | — | — | 1 | 8.26 |
| CHEMBL2021501 | — | — | 1 | 8.12 |
| CHEMBL2021493 | — | — | 1 | 7.96 |
| CHEMBL454621 | — | — | 1 | 7.96 |
| CHEMBL453620 | — | — | 1 | 7.85 |
| CHEMBL491327 | — | — | 1 | 7.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491326 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL512355 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL508331 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL452587 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL454620 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL523600 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2021502 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL489320 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL507804 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2021494 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL2021501 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL2021493 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL454621 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL453620 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL491327 | — | IC50 | = | 36.0 | nM | 7.44 |