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Assay Detail

CHEMBL643755

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Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.
Rosini M, Antonello A, Cavalli A, Bolognesi ML, Minarini A, Marucci G, Poggesi E, Leonardi A, Melchiorre C.
J Med Chem (2003) 46 : 4895 -4903
PubMed 14584940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.09 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25554 1 9.37
CHEMBL2 PRAZOSIN 4.0 1 9.23
CHEMBL2112853 1 7.50
CHEMBL143026 1 7.07
CHEMBL144286 1 7.02
CHEMBL423018 1 6.80
CHEMBL145785 1 6.54
CHEMBL143558 1 6.01
CHEMBL144779 1 5.77
CHEMBL145793 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25554 Ki = 0.4266 nM 9.37
CHEMBL2 PRAZOSIN Ki = 0.5888 nM 9.23
CHEMBL2112853 Ki = 31.62 nM 7.50
CHEMBL143026 Ki = 85.11 nM 7.07
CHEMBL144286 Ki = 95.5 nM 7.02
CHEMBL423018 Ki = 158.49 nM 6.80
CHEMBL145785 Ki = 288.4 nM 6.54
CHEMBL143558 Ki = 977.24 nM 6.01
CHEMBL144779 Ki = 1698.24 nM 5.77
CHEMBL145793 Ki = 2570.4 nM 5.59