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Assay Detail

CHEMBL637822

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

ADMET
Antagonist dissociation constant in rat spleen, number of determinations => 3.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Tissue Spleen
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 8.49 9.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 9.69
CHEMBL611 TERAZOSIN 4.0 1 8.60
CHEMBL709 ALFUZOSIN 4.0 1 8.31
CHEMBL290387 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN Kd = 0.2042 nM 9.69
CHEMBL611 TERAZOSIN Kd = 2.512 nM 8.60
CHEMBL709 ALFUZOSIN Kd = 4.898 nM 8.31
CHEMBL290387 Kd = 44.67 nM 7.35