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Assay Detail

CHEMBL913010

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Functional
Activity at adrenergic alpha 2A receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
7
Total Activities
7
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 Expert

Target

Alpha-2A adrenergic receptor (CHEMBL327)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).
Pallavicini M, Budriesi R, Fumagalli L, Ioan P, Chiarini A, Bolchi C, Ugenti MP, Colleoni S, Gobbi M, Valoti E.
J Med Chem (2006) 49 : 7140 -7149
PubMed 17125266 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.38 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215421 1 6.92
CHEMBL25554 1 6.59
CHEMBL214986 1 6.34
CHEMBL439346 1 6.20
CHEMBL217469 1 5.87
CHEMBL385371 1 -
CHEMBL215188 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215421 Kd = 120.23 nM 6.92
CHEMBL25554 Kd = 257.04 nM 6.59
CHEMBL214986 Kd = 457.09 nM 6.34
CHEMBL439346 Kd = 630.96 nM 6.20
CHEMBL217469 Kd = 1348.96 nM 5.87
CHEMBL385371 Kd > 10000.0 nM -
CHEMBL215188 Kd > 10000.0 nM -