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Assay Detail

CHEMBL875930

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Functional
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL319)
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 8 8.15 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL44403 1 9.46
CHEMBL25554 1 9.27
CHEMBL42472 1 8.95
CHEMBL43905 1 8.31
CHEMBL297106 1 8.23
CHEMBL42558 1 7.47
CHEMBL40325 1 6.97
CHEMBL42231 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL44403 Kd = 0.3467 nM 9.46
CHEMBL25554 Kd = 0.537 nM 9.27
CHEMBL42472 Kd = 1.122 nM 8.95
CHEMBL43905 Kd = 4.898 nM 8.31
CHEMBL297106 Kd = 5.888 nM 8.23
CHEMBL42558 Kd = 33.88 nM 7.47
CHEMBL40325 Kd = 107.15 nM 6.97
CHEMBL42231 Kd = 288.4 nM 6.54