Assay Detail
Binding
CHEMBL648618
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Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prostatic hyperplasia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 7.66 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | 8.10 |
| CHEMBL40650 | — | — | 1 | 7.78 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL40650 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL611 | TERAZOSIN | Ki | = | 78.0 | nM | 7.11 |