Assay Detail
Binding
CHEMBL831139
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Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells
25
Total Activities
25
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
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.01 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL537846 | — | — | 1 | 8.11 |
| CHEMBL367355 | — | — | 1 | 8.00 |
| CHEMBL360117 | — | — | 1 | 7.51 |
| CHEMBL181727 | — | — | 1 | 7.47 |
| CHEMBL182235 | — | — | 1 | 7.36 |
| CHEMBL362400 | — | — | 1 | 7.33 |
| CHEMBL180003 | — | — | 1 | 7.24 |
| CHEMBL181632 | — | — | 1 | 7.22 |
| CHEMBL359510 | — | — | 1 | 7.20 |
| CHEMBL360081 | — | — | 1 | 7.15 |
| CHEMBL179878 | — | — | 1 | 7.12 |
| CHEMBL181383 | — | — | 1 | 7.01 |
| CHEMBL180962 | — | — | 1 | 6.96 |
| CHEMBL362193 | — | — | 1 | 6.89 |
| CHEMBL181217 | — | — | 1 | 6.89 |
| CHEMBL181099 | — | — | 1 | 6.82 |
| CHEMBL361442 | — | — | 1 | 6.82 |
| CHEMBL360671 | — | — | 1 | 6.77 |
| CHEMBL178084 | — | — | 1 | 6.77 |
| CHEMBL360159 | — | — | 1 | 6.70 |
| CHEMBL182150 | — | — | 1 | 6.58 |
| CHEMBL181466 | — | — | 1 | 6.44 |
| CHEMBL181184 | — | — | 1 | 6.41 |
| CHEMBL360876 | — | — | 1 | 6.28 |
| CHEMBL181393 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL537846 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL367355 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL360117 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL181727 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL182235 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL362400 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL180003 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL181632 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL359510 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL360081 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL179878 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL181383 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL180962 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL362193 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL181217 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL181099 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL361442 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL360671 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL178084 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL360159 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL182150 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL181466 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL181184 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL360876 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL181393 | — | IC50 | = | 570.0 | nM | 6.24 |