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Assay Detail

CHEMBL646244

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

Binding
Compound was tested for binding affinity against native Alpha-1B adrenergic receptor from rat liver using radioligand ([3H]prazosin) binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-casein (CHEMBL2210)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
Giardinà D, Crucianelli M, Romanelli R, Leonardi A, Poggesi E, Melchiorre C.
J Med Chem (1996) 39 : 4602 -4607
PubMed 8917649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.12 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423294 CYCLAZOSIN 1 9.85
CHEMBL342062 1 9.68
CHEMBL97698 1 9.57
CHEMBL140450 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423294 CYCLAZOSIN Ki = 0.1413 nM 9.85
CHEMBL342062 Ki = 0.2089 nM 9.68
CHEMBL97698 Ki = 0.2692 nM 9.57
CHEMBL140450 Ki = 41.69 nM 7.38