Assay Detail
Binding
CHEMBL3583290
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.42 | 9.22 |
| Ki | 6 | 8.69 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3582270 | — | — | 2 | 9.52 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 2 | 9.22 |
| CHEMBL3582269 | — | — | 2 | 8.89 |
| CHEMBL3582268 | — | — | 2 | 8.68 |
| CHEMBL3582271 | — | — | 2 | 8.33 |
| CHEMBL3582272 | — | — | 2 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3582270 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3582270 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3582269 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3582268 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3582269 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3582268 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3582271 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL3582271 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3582272 | — | Ki | = | 29.9 | nM | 7.52 |
| CHEMBL3582272 | — | IC50 | = | 52.4 | nM | 7.28 |