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Assay Detail

CHEMBL644671

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

Functional
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
Minarini A, Budriesi R, Chiarini A, Leonardi A, Melchiorre C.
Bioorg Med Chem Lett (1998) 8 : 1353 -1358
PubMed 9871765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 7.56 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27013 1 9.04
CHEMBL2 PRAZOSIN 4.0 1 8.60
CHEMBL29591 1 7.53
CHEMBL423294 CYCLAZOSIN 1 7.48
CHEMBL543741 1 6.94
CHEMBL29907 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27013 Kd = 0.912 nM 9.04
CHEMBL2 PRAZOSIN Kd = 2.512 nM 8.60
CHEMBL29591 Kd = 29.51 nM 7.53
CHEMBL423294 CYCLAZOSIN Kd = 33.11 nM 7.48
CHEMBL543741 Kd = 114.82 nM 6.94
CHEMBL29907 Kd = 1778.28 nM 5.75