Assay Detail
Binding
CHEMBL649643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against alpha-2 adrenergic receptor using [3H]clonidine as radioligand in male Sprague-Dawley rats
7
Total Activities
7
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 | 7 | 5.95 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281864 | — | — | 1 | 6.64 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | — | 1 | 6.46 |
| CHEMBL26711 | — | — | 1 | 6.44 |
| CHEMBL28329 | — | — | 1 | 6.39 |
| CHEMBL27499 | — | — | 1 | 5.89 |
| CHEMBL25316 | — | — | 1 | 5.33 |
| CHEMBL27599 | — | — | 1 | 4.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281864 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL26711 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL28329 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL27499 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL25316 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL27599 | — | Ki | = | 34000.0 | nM | 4.47 |