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Assay Detail

CHEMBL670972

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

Binding
Compound was tested for binding affinity against native Dopamine receptor D2 from rat striatum using radioligand [3H]-spiperone)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
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 7.16 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 9.24
CHEMBL342062 1 5.08
CHEMBL2 PRAZOSIN 4.0 1 -
CHEMBL97698 1 -
CHEMBL423294 CYCLAZOSIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 0.5754 nM 9.24
CHEMBL342062 Ki = 8317.64 nM 5.08
CHEMBL2 PRAZOSIN Ki < 10000.0 nM -
CHEMBL97698 Ki < 10000.0 nM -
CHEMBL423294 CYCLAZOSIN Ki < 10000.0 nM -