Assay Detail
Binding
CHEMBL2060408
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Displacement of [3H]RX821001 from human alpha2B adrenoceptor expressed in CHO cells after 60 mins by gamma counter
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.29 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.50 |
| CHEMBL289480 | RILMENIDINE | 4.0 | 1 | 7.37 |
| CHEMBL2058633 | — | — | 1 | 6.03 |
| CHEMBL2058631 | — | — | 1 | 5.88 |
| CHEMBL2058632 | — | — | 1 | 5.55 |
| CHEMBL2058635 | — | — | 1 | 5.38 |
| CHEMBL2058634 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134 | CLONIDINE | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL289480 | RILMENIDINE | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL2058633 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL2058631 | — | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL2058632 | — | Ki | = | 2818.38 | nM | 5.55 |
| CHEMBL2058635 | — | Ki | = | 4168.69 | nM | 5.38 |
| CHEMBL2058634 | — | Ki | > | 10000.0 | nM | - |