Assay Detail
Binding
CHEMBL873170
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In vitro for binding affinity against Alpha-2 adrenergic receptor by radioligand [3H]clonidine in rat
11
Total Activities
11
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
Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 5.54 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | — | 1 | 6.46 |
| CHEMBL294079 | — | — | 1 | 6.28 |
| CHEMBL118475 | — | — | 1 | 6.09 |
| CHEMBL60434 | — | — | 1 | 6.08 |
| CHEMBL323692 | — | — | 1 | 5.58 |
| CHEMBL118420 | — | — | 1 | 5.39 |
| CHEMBL333343 | — | — | 1 | 5.34 |
| CHEMBL293023 | — | — | 1 | 5.21 |
| CHEMBL118310 | — | — | 1 | 4.96 |
| CHEMBL116945 | — | — | 1 | 4.80 |
| CHEMBL522 | BENZYLAMINE | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14346 | 1,2,3,4-TETRAHYDROISOQUINOLINE | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL294079 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL118475 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL60434 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL323692 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL118420 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL333343 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL293023 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL118310 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL116945 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL522 | BENZYLAMINE | Ki | = | 20000.0 | nM | 4.70 |