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Assay Detail

CHEMBL1060369

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

Binding
Displacement of [3H]prazosin from human alpha1A 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-1A adrenergic receptor (CHEMBL229)
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 8.40 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL707 DOXAZOSIN 4.0 1 9.27
CHEMBL561851 1 8.73
CHEMBL564481 CYCLODOXAZOSIN 1 8.55
CHEMBL558890 1 8.47
CHEMBL423294 CYCLAZOSIN 1 8.26
CHEMBL549764 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL707 DOXAZOSIN Ki = 0.537 nM 9.27
CHEMBL561851 Ki = 1.862 nM 8.73
CHEMBL564481 CYCLODOXAZOSIN Ki = 2.818 nM 8.55
CHEMBL558890 Ki = 3.388 nM 8.47
CHEMBL423294 CYCLAZOSIN Ki = 5.495 nM 8.26
CHEMBL549764 Ki = 81.28 nM 7.09