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Assay Detail

CHEMBL647543

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Ability to displace [3H]prazosin (0.25 nM) from whole brain of rat Alpha-1 adrenergic receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
Balle T, Perregaard J, Ramirez MT, Larsen AK, Søby KK, Liljefors T, Andersen K.
J Med Chem (2003) 46 : 265 -283
PubMed 12519065 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.10 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303313 1 9.35
CHEMBL64875 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303313 IC50 = 0.45 nM 9.35
CHEMBL64875 IC50 = 1.4 nM 8.85