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Assay Detail

CHEMBL2422343

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

Binding
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Prostate gland
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective α1D-adrenoceptor antagonist.
Fumagalli L, Pallavicini M, Budriesi R, Bolchi C, Canovi M, Chiarini A, Chiodini G, Gobbi M, Laurino P, Micucci M, Straniero V, Valoti E.
J Med Chem (2013) 56 : 6402 -6412
PubMed 23902232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 8.23 8.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2419769 1 8.71
CHEMBL3216590 1 8.44
CHEMBL2419765 1 7.88
CHEMBL2419771 1 7.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2419769 Kd = 1.95 nM 8.71
CHEMBL3216590 Kd = 3.631 nM 8.44
CHEMBL2419765 Kd = 13.18 nM 7.88
CHEMBL2419771 Kd = 13.18 nM 7.88