Assay Detail
Binding
CHEMBL648718
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Binding affinity to alpha-2 adrenergic receptor by displacement of [3H]clonidine
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 4.80 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287837 | — | — | 1 | 7.68 |
| CHEMBL38681 | — | — | 1 | 5.35 |
| CHEMBL39928 | — | — | 1 | 5.19 |
| CHEMBL6409 | CGS-19281A | — | 1 | 4.92 |
| CHEMBL59441 | — | — | 1 | 4.72 |
| CHEMBL320367 | — | — | 1 | 4.46 |
| CHEMBL95184 | — | — | 1 | 4.31 |
| CHEMBL97282 | — | — | 1 | 4.12 |
| CHEMBL95450 | — | — | 1 | 4.03 |
| CHEMBL316704 | — | — | 1 | 4.00 |
| CHEMBL26717 | — | — | 1 | 4.00 |
| CHEMBL40081 | — | — | 1 | - |
| CHEMBL95928 | — | — | 1 | - |
| CHEMBL41647 | — | — | 1 | - |
| CHEMBL95873 | — | — | 1 | - |
| CHEMBL318333 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287837 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL38681 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL39928 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL6409 | CGS-19281A | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL59441 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL320367 | — | Ki | = | 35000.0 | nM | 4.46 |
| CHEMBL95184 | — | Ki | = | 49000.0 | nM | 4.31 |
| CHEMBL97282 | — | Ki | = | 76000.0 | nM | 4.12 |
| CHEMBL95450 | — | Ki | = | 93000.0 | nM | 4.03 |
| CHEMBL316704 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL26717 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL40081 | — | Ki | = | 460000.0 | nM | - |
| CHEMBL95928 | — | Ki | = | 510000.0 | nM | - |
| CHEMBL41647 | — | Ki | = | 1400000.0 | nM | - |
| CHEMBL95873 | — | Ki | = | 680000.0 | nM | - |
| CHEMBL318333 | — | Ki | = | 680000.0 | nM | - |