Assay Detail
Binding
CHEMBL912585
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Inhibition of human 11beta-HSD1 over expressed in CHO cells by whole cell assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.48 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221749 | — | — | 1 | 8.40 |
| CHEMBL221083 | — | — | 1 | 8.00 |
| CHEMBL438654 | — | — | 1 | 7.75 |
| CHEMBL221477 | — | — | 1 | 7.75 |
| CHEMBL221084 | — | — | 1 | 7.75 |
| CHEMBL384653 | — | — | 1 | 7.75 |
| CHEMBL376470 | — | — | 1 | 7.70 |
| CHEMBL218006 | — | — | 1 | 7.48 |
| CHEMBL221391 | — | — | 1 | 7.40 |
| CHEMBL265625 | — | — | 1 | 7.39 |
| CHEMBL217983 | — | — | 1 | 7.28 |
| CHEMBL448483 | — | — | 1 | 7.25 |
| CHEMBL384684 | — | — | 1 | 7.02 |
| CHEMBL220742 | — | — | 1 | 6.77 |
| CHEMBL220816 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221749 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL221083 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL438654 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL221477 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL221084 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL384653 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL376470 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL218006 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL221391 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL265625 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL217983 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL448483 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL384684 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL220742 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL220816 | — | IC50 | = | 268.0 | nM | 6.57 |