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Assay Detail

CHEMBL645198

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Functional
Antagonistic affinity tested against isolated Rat Thoracic Aorta Alpha-1D adrenergic receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1D adrenergic receptor (CHEMBL326)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.
Quaglia W, Pigini M, Piergentili A, Giannella M, Gentili F, Marucci G, Carrieri A, Carotti A, Poggesi E, Leonardi A, Melchiorre C.
J Med Chem (2002) 45 : 1633 -1643
PubMed 11931617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 8.08 9.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42472 1 9.56
CHEMBL25554 1 8.80
CHEMBL44403 1 8.70
CHEMBL13647 BMY-7378 1 8.40
CHEMBL42558 1 7.78
CHEMBL43905 1 7.76
CHEMBL297106 1 7.49
CHEMBL40325 1 7.21
CHEMBL42231 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42472 Kd = 0.2754 nM 9.56
CHEMBL25554 Kd = 1.585 nM 8.80
CHEMBL44403 Kd = 1.995 nM 8.70
CHEMBL13647 BMY-7378 Kd = 3.981 nM 8.40
CHEMBL42558 Kd = 16.6 nM 7.78
CHEMBL43905 Kd = 17.38 nM 7.76
CHEMBL297106 Kd = 32.36 nM 7.49
CHEMBL40325 Kd = 61.66 nM 7.21
CHEMBL42231 Kd = 91.2 nM 7.04