Assay Detail
Binding
CHEMBL648470
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Alpha-2 adrenergic receptor binding affinity by measuring the displacement of [3H]clonidine binding in rat cerebral cortex
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.09 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341723 | — | — | 1 | 7.50 |
| CHEMBL140477 | — | — | 1 | 7.00 |
| CHEMBL142912 | — | — | 1 | 7.00 |
| CHEMBL141194 | — | — | 1 | 6.43 |
| CHEMBL143397 | — | — | 1 | 6.36 |
| CHEMBL143463 | — | — | 1 | 6.28 |
| CHEMBL142995 | — | — | 1 | 5.82 |
| CHEMBL142635 | NAFTOPIDIL | 4.0 | 1 | 5.80 |
| CHEMBL143288 | — | — | 1 | 5.77 |
| CHEMBL142859 | — | — | 1 | 5.64 |
| CHEMBL142948 | — | — | 1 | 5.52 |
| CHEMBL142474 | — | — | 1 | 5.48 |
| CHEMBL143944 | — | — | 1 | 5.34 |
| CHEMBL143923 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341723 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL140477 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL142912 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL141194 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL143397 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL143463 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL142995 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL142635 | NAFTOPIDIL | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL143288 | — | Ki | = | 1706.0 | nM | 5.77 |
| CHEMBL142859 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL142948 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL142474 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL143944 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL143923 | — | Ki | = | 4600.0 | nM | 5.34 |