Assay Detail
ADMET
CHEMBL4041723
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Displacement of [3H]prazosin from recombinant human alpha-1a adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.84 | 7.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2312227 | — | — | 1 | 7.56 |
| CHEMBL4075507 | — | — | 1 | 6.94 |
| CHEMBL4067083 | — | — | 1 | 6.93 |
| CHEMBL4091168 | — | — | 1 | 6.81 |
| CHEMBL4070363 | — | — | 1 | 6.77 |
| CHEMBL4082195 | — | — | 1 | 6.71 |
| CHEMBL4071929 | — | — | 1 | 6.55 |
| CHEMBL13647 | BMY-7378 | — | 1 | 6.42 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2312227 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL4075507 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL4067083 | — | Ki | = | 117.49 | nM | 6.93 |
| CHEMBL4091168 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL4070363 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL4082195 | — | Ki | = | 194.98 | nM | 6.71 |
| CHEMBL4071929 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL13647 | BMY-7378 | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL56 | 8-OH-DPAT | Ki | > | 1000.0 | nM | - |