Assay Detail
Binding
CHEMBL831429
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Inhibitory activity against constitutively activated human Alpha-2A adrenergic receptor transiently expressed in COS-1 cells using [3H]MK-912
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.26 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL194173 | — | — | 1 | 8.25 |
| CHEMBL193438 | — | — | 1 | 8.11 |
| CHEMBL193970 | — | — | 1 | 7.68 |
| CHEMBL193771 | — | — | 1 | 7.33 |
| CHEMBL193666 | — | — | 1 | 7.24 |
| CHEMBL195346 | — | — | 1 | 7.24 |
| CHEMBL195123 | — | — | 1 | 7.07 |
| CHEMBL17645 | CGP-71683A | — | 1 | 7.01 |
| CHEMBL192266 | — | — | 1 | 7.00 |
| CHEMBL194602 | — | — | 1 | 6.96 |
| CHEMBL195810 | — | — | 1 | 6.89 |
| CHEMBL425012 | — | — | 1 | 6.85 |
| CHEMBL360671 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL194173 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL193438 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL193970 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL193771 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL193666 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL195346 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL195123 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL17645 | CGP-71683A | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL192266 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL194602 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL195810 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL425012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL360671 | — | IC50 | = | 170.0 | nM | 6.77 |