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Assay Detail

CHEMBL798079

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

Functional
Alpha-1-Adrenoceptor blocking activity as antagonism of (-)-norepinephrine induced contractions of epididymal vas deferens
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Vas deferens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity relationships for prazosin and WB 4101 analogues as alpha 1-adrenoreceptor antagonists.
Giardinà D, Bertini R, Brancia E, Brasili L, Melchiorre C.
J Med Chem (1985) 28 : 1354 -1357
PubMed 2863379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 7.80 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL556001 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) 1 8.83
CHEMBL538219 1 8.81
CHEMBL1558 PRAZOSIN HYDROCHLORIDE 4.0 1 8.74
CHEMBL542075 1 7.88
CHEMBL545387 1 7.86
CHEMBL543984 1 7.22
CHEMBL554232 1 7.19
CHEMBL555983 1 7.18
CHEMBL544221 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL556001 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) Kd = 1.479 nM 8.83
CHEMBL538219 Kd = 1.549 nM 8.81
CHEMBL1558 PRAZOSIN HYDROCHLORIDE Kd = 1.82 nM 8.74
CHEMBL542075 Kd = 13.18 nM 7.88
CHEMBL545387 Kd = 13.8 nM 7.86
CHEMBL543984 Kd = 60.26 nM 7.22
CHEMBL554232 Kd = 64.57 nM 7.19
CHEMBL555983 Kd = 66.07 nM 7.18
CHEMBL544221 Kd = 354.81 nM 6.45