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Assay Detail

CHEMBL646228

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Functional
Antagonistic affinity tested against isolated Rat Spleen Alpha-1B adrenergic receptor
9
Total Activities
9
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-1B adrenergic receptor (CHEMBL315)
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 7.09 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25554 1 8.16
CHEMBL44403 1 7.58
CHEMBL42472 1 7.54
CHEMBL13647 BMY-7378 1 7.48
CHEMBL42558 1 7.17
CHEMBL42231 1 6.96
CHEMBL43905 1 6.81
CHEMBL40325 1 6.52
CHEMBL297106 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25554 Kd = 6.918 nM 8.16
CHEMBL44403 Kd = 26.3 nM 7.58
CHEMBL42472 Kd = 28.84 nM 7.54
CHEMBL13647 BMY-7378 Kd = 33.11 nM 7.48
CHEMBL42558 Kd = 67.61 nM 7.17
CHEMBL42231 Kd = 109.65 nM 6.96
CHEMBL43905 Kd = 154.88 nM 6.81
CHEMBL40325 Kd = 302.0 nM 6.52
CHEMBL297106 Kd = 2511.89 nM 5.60