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Assay Detail

CHEMBL645513

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

Functional
Alpha-2 adrenergic receptor blocking activity by antagonism of clonidine induced depression of twitch response of field stimulated prostatic portion of rat vas deferens
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity relationships among benextramine-related tetraamine disulfides. Chain length effect on alpha-adrenoreceptor blocking activity.
Quaglia W, Brasili L, Cristalli G, Giardinà D, Picchio MT, Melchiorre C.
J Med Chem (1988) 31 : 1861 -1866
PubMed 2900899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.64 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19060 BENEXTRAMINE 1 6.09
CHEMBL55957 1 5.98
CHEMBL299486 1 5.91
CHEMBL301293 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19060 BENEXTRAMINE IC50 = 820.0 nM 6.09
CHEMBL55957 IC50 = 1040.0 nM 5.98
CHEMBL299486 IC50 = 1220.0 nM 5.91
CHEMBL301293 IC50 = 25800.0 nM 4.59