Assay Detail
Binding
CHEMBL828282
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In vitro inhibition of [3H]clonidine from alpha-2 adrenergic receptor of rat cortex
17
Total Activities
17
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
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 5.35 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL287837 | — | — | 1 | 7.68 |
| CHEMBL121531 | — | — | 1 | 5.42 |
| CHEMBL176112 | — | — | 1 | 4.28 |
| CHEMBL26717 | — | — | 1 | 4.00 |
| CHEMBL95873 | — | — | 1 | - |
| CHEMBL41647 | — | — | 1 | - |
| CHEMBL177861 | — | — | 1 | - |
| CHEMBL435536 | — | — | 1 | - |
| CHEMBL355581 | — | — | 1 | - |
| CHEMBL290890 | — | — | 1 | - |
| CHEMBL178695 | — | — | 1 | - |
| CHEMBL177621 | — | — | 1 | - |
| CHEMBL175527 | — | — | 1 | - |
| CHEMBL177062 | — | — | 1 | - |
| CHEMBL175935 | — | — | 1 | - |
| CHEMBL366785 | — | — | 1 | - |
| CHEMBL175519 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL287837 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL121531 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL176112 | — | Ki | = | 53000.0 | nM | 4.28 |
| CHEMBL26717 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL95873 | — | Ki | = | 680000.0 | nM | - |
| CHEMBL41647 | — | Ki | = | 1400000.0 | nM | - |
| CHEMBL177861 | — | Ki | = | 550000.0 | nM | - |
| CHEMBL435536 | — | Ki | = | 610000.0 | nM | - |
| CHEMBL355581 | — | Ki | = | 190000.0 | nM | - |
| CHEMBL290890 | — | Ki | = | 140000.0 | nM | - |
| CHEMBL178695 | — | Ki | = | 1200000.0 | nM | - |
| CHEMBL177621 | — | Ki | = | 660000.0 | nM | - |
| CHEMBL175527 | — | Ki | = | 210000.0 | nM | - |
| CHEMBL177062 | — | Ki | = | 230000.0 | nM | - |
| CHEMBL175935 | — | Ki | = | 320000.0 | nM | - |
| CHEMBL366785 | — | Ki | = | 340000.0 | nM | - |
| CHEMBL175519 | — | Ki | = | 520000.0 | nM | - |