Assay Detail
Binding
CHEMBL647724
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In vitro binding affinity to the human alpha-2A adrenergic receptor
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 8.59 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419316 | — | — | 1 | 9.52 |
| CHEMBL319119 | — | — | 1 | 9.52 |
| CHEMBL100879 | — | — | 1 | 9.52 |
| CHEMBL319530 | — | — | 1 | 9.30 |
| CHEMBL91157 | — | — | 1 | 9.10 |
| CHEMBL99868 | — | — | 1 | 9.00 |
| CHEMBL263424 | — | — | 1 | 8.96 |
| CHEMBL101596 | — | — | 1 | 8.96 |
| CHEMBL328195 | — | — | 1 | 8.85 |
| CHEMBL99916 | — | — | 1 | 8.77 |
| CHEMBL98646 | — | — | 1 | 8.77 |
| CHEMBL329065 | — | — | 1 | 8.72 |
| CHEMBL319573 | — | — | 1 | 8.54 |
| CHEMBL98541 | — | — | 1 | 8.54 |
| CHEMBL419336 | — | — | 1 | 8.52 |
| CHEMBL318235 | — | — | 1 | 8.47 |
| CHEMBL101361 | — | — | 1 | 8.28 |
| CHEMBL95218 | — | — | 1 | 8.23 |
| CHEMBL328114 | — | — | 1 | 8.06 |
| CHEMBL419894 | — | — | 1 | 8.05 |
| CHEMBL328631 | — | — | 1 | 8.03 |
| CHEMBL98889 | — | — | 1 | 7.66 |
| CHEMBL420830 | — | — | 1 | 7.64 |
| CHEMBL101411 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419316 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL319119 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL100879 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL319530 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL91157 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL99868 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL263424 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL101596 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL328195 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL99916 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL98646 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL329065 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL319573 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL98541 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL419336 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL318235 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL101361 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL95218 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL328114 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL419894 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL328631 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL98889 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL420830 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL101411 | — | Ki | = | 69.0 | nM | 7.16 |