Assay Detail
Binding
CHEMBL891018
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Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.78 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL243694 | — | — | 2 | 9.70 |
| CHEMBL8618 | NAN-190 | — | 1 | 9.59 |
| CHEMBL243229 | — | — | 1 | 9.40 |
| CHEMBL243228 | — | — | 1 | 9.10 |
| CHEMBL243864 | — | — | 1 | 8.74 |
| CHEMBL243692 | — | — | 1 | 8.57 |
| CHEMBL243866 | — | — | 2 | 8.41 |
| CHEMBL243690 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL243694 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL8618 | NAN-190 | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL243229 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL243228 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL243694 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL243864 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL243692 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL243866 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL243866 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL243690 | — | Ki | = | 37.8 | nM | 7.42 |