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Assay Detail

CHEMBL873450

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

Functional
In vitro antagonistic activity against alpha-1A receptor in dog prostate.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Tissue Prostate gland
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
Meyer MD, Altenbach RJ, Bai H, Basha FZ, Carroll WA, Kerwin JF, Lebold SA, Lee E, Pratt JK, Sippy KB, Tietje K, Wendt MD, Brune ME, Buckner SA, Hancock AA, Drizin I.
J Med Chem (2001) 44 : 1971 -1985
PubMed 11384242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 8.59 9.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62033 1 9.83
CHEMBL836 TAMSULOSIN 4.0 1 9.54
CHEMBL293695 1 9.45
CHEMBL445325 1 9.23
CHEMBL291303 1 9.01
CHEMBL707 DOXAZOSIN 4.0 1 7.59
CHEMBL611 TERAZOSIN 4.0 1 7.44
CHEMBL709 ALFUZOSIN 4.0 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62033 Kd = 0.1479 nM 9.83
CHEMBL836 TAMSULOSIN Kd = 0.2884 nM 9.54
CHEMBL293695 Kd = 0.3548 nM 9.45
CHEMBL445325 Kd = 0.5888 nM 9.23
CHEMBL291303 Kd = 0.9772 nM 9.01
CHEMBL707 DOXAZOSIN Kd = 25.7 nM 7.59
CHEMBL611 TERAZOSIN Kd = 36.31 nM 7.44
CHEMBL709 ALFUZOSIN Kd = 218.78 nM 6.66