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Assay Detail

CHEMBL616340

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

Binding
Binding affinity against native 5-HT1A-receptors from rat hippocampus using radioligand ([3H]8-hydroxy-2-(di-n-propylamino)-tetraline) binding assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
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 5 5.70 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 7.60
CHEMBL2 PRAZOSIN 4.0 1 5.63
CHEMBL423294 CYCLAZOSIN 1 5.21
CHEMBL97698 1 5.16
CHEMBL342062 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 25.12 nM 7.60
CHEMBL2 PRAZOSIN Ki = 2344.23 nM 5.63
CHEMBL423294 CYCLAZOSIN Ki = 6165.95 nM 5.21
CHEMBL97698 Ki = 6918.31 nM 5.16
CHEMBL342062 Ki = 12882.5 nM 4.89