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Assay Detail

CHEMBL637823

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ADMET
Antagonist dissociation constant in rat vas deferens
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Tissue Vas deferens
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Meyer MD, Altenbach RJ, Basha FZ, Carroll WA, Condon S, Elmore SW, Kerwin JF, Sippy KB, Tietje K, Wendt MD, Hancock AA, Brune ME, Buckner SA, Drizin I.
J Med Chem (2000) 43 : 1586 -1603
PubMed 10780916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 8.75 8.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40650 1 8.93
CHEMBL2112073 1 8.71
CHEMBL707 DOXAZOSIN 4.0 1 8.69
CHEMBL291262 1 8.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40650 Kd = 1.175 nM 8.93
CHEMBL2112073 Kd = 1.95 nM 8.71
CHEMBL707 DOXAZOSIN Kd = 2.042 nM 8.69
CHEMBL291262 Kd = 2.239 nM 8.65