Assay Detail
Binding
CHEMBL649642
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In vitro inhibitory activity against Alpha-2 adrenergic receptor using [3H]clonidine as radioligand in male Sprague-Dawley rats
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and the alpha2-adrenoceptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 5.07 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26828 | — | — | 1 | 6.66 |
| CHEMBL26640 | — | — | 1 | 6.33 |
| CHEMBL27730 | — | — | 1 | 5.66 |
| CHEMBL286495 | — | — | 1 | 5.64 |
| CHEMBL28340 | — | — | 1 | 5.51 |
| CHEMBL281289 | — | — | 1 | 5.37 |
| CHEMBL26825 | — | — | 1 | 5.34 |
| CHEMBL26879 | — | — | 1 | 5.21 |
| CHEMBL286497 | — | — | 1 | 5.20 |
| CHEMBL27162 | — | — | 1 | 5.14 |
| CHEMBL26667 | — | — | 1 | 5.04 |
| CHEMBL27776 | — | — | 1 | 4.96 |
| CHEMBL143953 | — | — | 1 | 4.92 |
| CHEMBL28115 | — | — | 1 | 4.75 |
| CHEMBL28431 | — | — | 1 | 4.68 |
| CHEMBL28228 | — | — | 1 | 4.64 |
| CHEMBL441679 | — | — | 1 | 4.57 |
| CHEMBL28390 | — | — | 1 | 4.50 |
| CHEMBL27954 | — | — | 1 | 4.29 |
| CHEMBL280592 | — | — | 1 | 4.02 |
| CHEMBL26717 | — | — | 1 | 4.00 |
| CHEMBL27664 | — | — | 1 | - |
| CHEMBL27639 | — | — | 1 | - |
| CHEMBL341882 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26828 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL26640 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL27730 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL286495 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL28340 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL281289 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL26825 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL26879 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL286497 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL27162 | — | Ki | = | 7300.0 | nM | 5.14 |
| CHEMBL26667 | — | Ki | = | 9100.0 | nM | 5.04 |
| CHEMBL27776 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL143953 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL28115 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL28431 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL28228 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL441679 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL28390 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL27954 | — | Ki | = | 51000.0 | nM | 4.29 |
| CHEMBL280592 | — | Ki | = | 95000.0 | nM | 4.02 |
| CHEMBL26717 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL27664 | — | Ki | = | 160000.0 | nM | - |
| CHEMBL27639 | — | Ki | = | 190000.0 | nM | - |
| CHEMBL341882 | — | Ki | = | 470000.0 | nM | - |