Assay Detail
Binding
CHEMBL855996
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Inhibition of human 11beta-HSD1 expressed in HEK cells
18
Total Activities
17
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 | Intermediate |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.74 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219448 | — | — | 1 | 8.10 |
| CHEMBL219295 | — | — | 1 | 7.66 |
| CHEMBL219403 | — | — | 2 | 7.19 |
| CHEMBL384426 | — | — | 1 | 7.14 |
| CHEMBL216783 | — | — | 1 | 7.12 |
| CHEMBL386315 | — | — | 1 | 7.10 |
| CHEMBL375743 | — | — | 1 | 6.73 |
| CHEMBL3085038 | — | — | 1 | 6.70 |
| CHEMBL218246 | — | — | 1 | 6.66 |
| CHEMBL218247 | — | — | 1 | 6.36 |
| CHEMBL219606 | — | — | 1 | 6.35 |
| CHEMBL374409 | — | — | 1 | 6.22 |
| CHEMBL387010 | — | — | 1 | 6.20 |
| CHEMBL376272 | — | — | 1 | 5.62 |
| CHEMBL387424 | — | — | 1 | - |
| CHEMBL386947 | — | — | 1 | - |
| CHEMBL384692 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219448 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL219295 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL219403 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL384426 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL216783 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL386315 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL375743 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL3085038 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL218246 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL218247 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL219606 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL374409 | — | IC50 | = | 606.0 | nM | 6.22 |
| CHEMBL387010 | — | IC50 | = | 637.0 | nM | 6.20 |
| CHEMBL219403 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL376272 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL387424 | — | IC50 | - | — | - | |
| CHEMBL386947 | — | IC50 | - | — | - | |
| CHEMBL384692 | — | IC50 | - | — | - |