Assay Detail
Binding
CHEMBL1037060
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Displacement of [3H]MK-912 from human adrenergic alpha2A receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.40 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182150 | — | — | 1 | 6.98 |
| CHEMBL568400 | — | — | 1 | 6.89 |
| CHEMBL583014 | — | — | 1 | 6.70 |
| CHEMBL577904 | — | — | 1 | 6.68 |
| CHEMBL566075 | — | — | 1 | 6.51 |
| CHEMBL565551 | — | — | 1 | 6.33 |
| CHEMBL567993 | — | — | 1 | 6.24 |
| CHEMBL567791 | — | — | 1 | 6.14 |
| CHEMBL577912 | — | — | 1 | 5.80 |
| CHEMBL578170 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182150 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL568400 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL583014 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL577904 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL566075 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL565551 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL567993 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL567791 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL577912 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL578170 | — | IC50 | = | 1770.0 | nM | 5.75 |