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Assay Detail

CHEMBL4041732

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

ADMET
Displacement of [3H]N-methylspiperone from recombinant human D3 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes.
Del Bello F, Bonifazi A, Giannella M, Giorgioni G, Piergentili A, Petrelli R, Cifani C, Micioni Di Bonaventura MV, Keck TM, Mazzolari A, Vistoli G, Cilia A, Poggesi E, Matucci R, Quaglia W.
Eur J Med Chem (2017) 125 : 233 -244
PubMed 27662034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.51 7.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2312227 1 7.88
CHEMBL4082195 1 7.47
CHEMBL4071929 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2312227 Ki = 13.18 nM 7.88
CHEMBL4082195 Ki = 33.88 nM 7.47
CHEMBL4071929 Ki = 66.07 nM 7.18