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Assay Detail

CHEMBL648101

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

Binding
Compound was tested for binding affinity against cloned Alpha-1B adrenergic receptor from hamster smooth muscle using radioligand ([3H]prazosin) binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

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 6 8.80 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423294 CYCLAZOSIN 1 9.51
CHEMBL2 PRAZOSIN 4.0 1 9.34
CHEMBL97698 1 9.23
CHEMBL342062 1 9.16
CHEMBL267930 SPIPERONE 2.0 1 8.15
CHEMBL140450 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423294 CYCLAZOSIN Ki = 0.309 nM 9.51
CHEMBL2 PRAZOSIN Ki = 0.4571 nM 9.34
CHEMBL97698 Ki = 0.5888 nM 9.23
CHEMBL342062 Ki = 0.6918 nM 9.16
CHEMBL267930 SPIPERONE Ki = 7.079 nM 8.15
CHEMBL140450 Ki = 39.81 nM 7.40