Assay Detail
Binding
CHEMBL903400
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Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HepG2 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.10 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL394218 | — | — | 1 | 9.10 |
| CHEMBL537669 | YOHIMBINE HYDROCHLORIDE | 3.0 | 1 | 8.72 |
| CHEMBL247665 | — | — | 1 | 8.46 |
| CHEMBL247664 | — | — | 1 | 8.38 |
| CHEMBL392991 | — | — | 1 | 8.10 |
| CHEMBL428407 | — | — | 1 | 8.03 |
| CHEMBL392771 | — | — | 1 | 8.03 |
| CHEMBL246229 | — | — | 1 | 8.02 |
| CHEMBL393597 | — | — | 1 | 7.96 |
| CHEMBL246852 | — | — | 1 | 7.75 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 7.72 |
| CHEMBL246639 | — | — | 1 | 7.72 |
| CHEMBL246228 | — | — | 1 | 7.72 |
| CHEMBL392992 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL394218 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL537669 | YOHIMBINE HYDROCHLORIDE | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL247665 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL247664 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL392991 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL428407 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL392771 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL246229 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL393597 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL246852 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL246639 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL246228 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL392992 | — | Ki | = | 20.0 | nM | 7.70 |