Assay Detail
Binding
CHEMBL644760
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In vitro binding affinity towards human alpha-2B adrenergic receptor using [3H]rauwolscine
26
Total Activities
22
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 alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.43 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90943 | — | — | 1 | 8.70 |
| CHEMBL91157 | — | — | 2 | 8.52 |
| CHEMBL93171 | — | — | 1 | 8.12 |
| CHEMBL268258 | — | — | 1 | 7.96 |
| CHEMBL422597 | — | — | 1 | 7.92 |
| CHEMBL419316 | — | — | 2 | 7.85 |
| CHEMBL92860 | — | — | 2 | 7.85 |
| CHEMBL328114 | — | — | 2 | 7.85 |
| CHEMBL90247 | — | — | 1 | 7.80 |
| CHEMBL90997 | — | — | 1 | 7.64 |
| CHEMBL327875 | — | — | 1 | 7.51 |
| CHEMBL93489 | — | — | 1 | 7.38 |
| CHEMBL90419 | — | — | 1 | 7.38 |
| CHEMBL94129 | — | — | 1 | 7.31 |
| CHEMBL328377 | — | — | 1 | 6.50 |
| CHEMBL93801 | — | — | 1 | 6.43 |
| CHEMBL90966 | — | — | 1 | 6.14 |
| CHEMBL90843 | — | — | 1 | 6.00 |
| CHEMBL92496 | — | — | 1 | - |
| CHEMBL91297 | — | — | 1 | - |
| CHEMBL91824 | — | — | 1 | - |
| CHEMBL94435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90943 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL91157 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL93171 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL268258 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL422597 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL419316 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL92860 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL328114 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL91157 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL90247 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL90997 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL327875 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL90419 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL93489 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL328114 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL94129 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL92860 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL328377 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL93801 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL419316 | — | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL90966 | — | Ki | = | 721.0 | nM | 6.14 |
| CHEMBL90843 | — | Ki | = | 995.0 | nM | 6.00 |
| CHEMBL92496 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL91824 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL91297 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL94435 | — | Ki | > | 1000.0 | nM | - |