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Assay Detail

CHEMBL645569

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Binding
Binding affinity measured in CHO cells expressing human cloned Alpha-1B adrenergic receptor expressed as pKi
6
Total Activities
6
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-1B adrenergic receptor (CHEMBL232)
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 6 7.42 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143026 1 8.05
CHEMBL25554 1 8.00
CHEMBL2112853 1 7.90
CHEMBL143558 1 7.40
CHEMBL144779 1 6.66
CHEMBL145793 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143026 Ki = 8.913 nM 8.05
CHEMBL25554 Ki = 10.0 nM 8.00
CHEMBL2112853 Ki = 12.59 nM 7.90
CHEMBL143558 Ki = 39.81 nM 7.40
CHEMBL144779 Ki = 218.78 nM 6.66
CHEMBL145793 Ki = 295.12 nM 6.53