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Assay Detail

CHEMBL670916

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

Functional
In vivo antagonist dissociation constant in intaraurethral pressure model in dogs.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Confidence 1 — Organism
Curated By Intermediate

Target

Canis familiaris (CHEMBL373)
Type ORGANISM
Organism Canis lupus familiaris

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 5 7.64 8.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 8.87
CHEMBL445325 1 8.30
CHEMBL707 DOXAZOSIN 4.0 1 7.12
CHEMBL611 TERAZOSIN 4.0 1 7.02
CHEMBL709 ALFUZOSIN 4.0 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN Kd = 1.349 nM 8.87
CHEMBL445325 Kd = 5.012 nM 8.30
CHEMBL707 DOXAZOSIN Kd = 75.86 nM 7.12
CHEMBL611 TERAZOSIN Kd = 95.5 nM 7.02
CHEMBL709 ALFUZOSIN Kd = 134.9 nM 6.87