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Assay Detail

CHEMBL1060370

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]prazosin from human Alpha-1B adrenoceptor expressed in CHO cells
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 Intermediate

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
Giardinà D, Martarelli D, Sagratini G, Angeli P, Ballinari D, Gulini U, Melchiorre C, Poggesi E, Pompei P.
J Med Chem (2009) 52 : 4951 -4954
PubMed 19719240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.92 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423294 CYCLAZOSIN 1 9.49
CHEMBL564481 CYCLODOXAZOSIN 1 9.38
CHEMBL707 DOXAZOSIN 4.0 1 9.09
CHEMBL561851 1 9.03
CHEMBL558890 1 8.85
CHEMBL549764 1 7.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423294 CYCLAZOSIN Ki = 0.3236 nM 9.49
CHEMBL564481 CYCLODOXAZOSIN Ki = 0.4169 nM 9.38
CHEMBL707 DOXAZOSIN Ki = 0.8128 nM 9.09
CHEMBL561851 Ki = 0.9333 nM 9.03
CHEMBL558890 Ki = 1.413 nM 8.85
CHEMBL549764 Ki = 22.39 nM 7.65