Assay Detail
Binding
CHEMBL649629
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Inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 5.46 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130744 | — | — | 1 | 7.11 |
| CHEMBL338311 | — | — | 1 | 6.08 |
| CHEMBL128633 | — | — | 1 | 5.80 |
| CHEMBL131174 | — | — | 1 | 5.68 |
| CHEMBL27730 | — | — | 1 | 5.66 |
| CHEMBL131412 | — | — | 1 | 5.34 |
| CHEMBL286497 | — | — | 1 | 5.20 |
| CHEMBL27776 | — | — | 1 | 4.96 |
| CHEMBL28115 | — | — | 1 | 4.75 |
| CHEMBL26717 | — | — | 1 | 4.00 |
| CHEMBL39125 | — | — | 1 | - |
| CHEMBL27639 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130744 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL338311 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL128633 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL131174 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL27730 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL131412 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL286497 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL27776 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL28115 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL26717 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL39125 | — | Ki | = | 130000.0 | nM | - |
| CHEMBL27639 | — | Ki | = | 190000.0 | nM | - |