Assay Detail
ADMET
CHEMBL4041722
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Displacement of [3H]prazosin from recombinant human alpha-1b 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 | 6.70 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2312227 | — | — | 1 | 7.25 |
| CHEMBL4091168 | — | — | 1 | 6.94 |
| CHEMBL4075507 | — | — | 1 | 6.92 |
| CHEMBL4070363 | — | — | 1 | 6.75 |
| CHEMBL4067083 | — | — | 1 | 6.60 |
| CHEMBL4071929 | — | — | 1 | 6.54 |
| CHEMBL4082195 | — | — | 1 | 6.43 |
| CHEMBL13647 | BMY-7378 | — | 1 | 6.15 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2312227 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL4091168 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL4075507 | — | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL4070363 | — | Ki | = | 177.83 | nM | 6.75 |
| CHEMBL4067083 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL4071929 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL4082195 | — | Ki | = | 371.54 | nM | 6.43 |
| CHEMBL13647 | BMY-7378 | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL56 | 8-OH-DPAT | Ki | > | 1000.0 | nM | - |