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Assay Detail

CHEMBL891167

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

Binding
Displacement of [3H]prazosin from human adrenergic alpha-1b receptor expressed in CHO cells
9
Total Activities
9
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

Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
Sagratini G, Angeli P, Buccioni M, Gulini U, Marucci G, Melchiorre C, Leonardi A, Poggesi E, Giardinà D.
Bioorg Med Chem (2007) 15 : 2334 -2345
PubMed 17276073 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 9.11 9.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423294 CYCLAZOSIN 1 9.87
CHEMBL242724 1 9.62
CHEMBL388884 1 9.51
CHEMBL242934 1 9.31
CHEMBL242508 1 9.06
CHEMBL242507 1 9.06
CHEMBL242723 1 8.86
CHEMBL389978 1 8.50
CHEMBL242725 1 8.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423294 CYCLAZOSIN Ki = 0.1349 nM 9.87
CHEMBL242724 Ki = 0.2399 nM 9.62
CHEMBL388884 Ki = 0.309 nM 9.51
CHEMBL242934 Ki = 0.4898 nM 9.31
CHEMBL242508 Ki = 0.871 nM 9.06
CHEMBL242507 Ki = 0.871 nM 9.06
CHEMBL242723 Ki = 1.38 nM 8.86
CHEMBL389978 Ki = 3.162 nM 8.50
CHEMBL242725 Ki = 5.888 nM 8.23