Assay Detail
Binding
CHEMBL652817
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Binding affinity for human Alpha-1A adrenergic receptor expressed in COS cell membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.50 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12062 | RWJ-69736 | — | 1 | 9.18 |
| CHEMBL275469 | RWJ-38063 | — | 1 | 8.06 |
| CHEMBL12603 | RWJ-68157 | — | 1 | 7.75 |
| CHEMBL12127 | — | — | 1 | 7.75 |
| CHEMBL12529 | — | — | 1 | 7.70 |
| CHEMBL11828 | — | — | 1 | 7.55 |
| CHEMBL12202 | — | — | 1 | 7.42 |
| CHEMBL268030 | — | — | 1 | 7.28 |
| CHEMBL418531 | — | — | 1 | 7.08 |
| CHEMBL12501 | — | — | 1 | 7.01 |
| CHEMBL12364 | — | — | 1 | 6.89 |
| CHEMBL274529 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12062 | RWJ-69736 | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL275469 | RWJ-38063 | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL12603 | RWJ-68157 | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL12127 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL12529 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL11828 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL12202 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL268030 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL418531 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL12501 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL12364 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL274529 | — | Ki | = | 417.0 | nM | 6.38 |