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Assay Detail

CHEMBL2155388

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

Functional
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Vas deferens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selective α1B-adrenoceptor antagonist.
Fumagalli L, Pallavicini M, Budriesi R, Gobbi M, Straniero V, Zagami M, Chiodini G, Bolchi C, Chiarini A, Micucci M, Valoti E.
Eur J Med Chem (2012) 58 : 184 -191
PubMed 23124215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 8.32 9.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215421 1 9.98
CHEMBL2153555 1 9.56
CHEMBL2153553 1 8.77
CHEMBL2153557 1 7.54
CHEMBL2153559 1 7.27
CHEMBL2153551 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215421 Kd = 0.1047 nM 9.98
CHEMBL2153555 Kd = 0.2754 nM 9.56
CHEMBL2153553 Kd = 1.698 nM 8.77
CHEMBL2153557 Kd = 28.84 nM 7.54
CHEMBL2153559 Kd = 53.7 nM 7.27
CHEMBL2153551 Kd = 165.96 nM 6.78