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Assay Detail

CHEMBL3270695

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Binding
Antagonist activity at human dopamine D3 receptor expressed in human U2OS cells assessed as inhibition of pramipexole-stimulated beta-arrestin recruitment
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.
Chen J, Levant B, Jiang C, Keck TM, Newman AH, Wang S.
J Med Chem (2014) 57 : 4962 -4968
PubMed 24848155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.19 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540612 1 7.89
CHEMBL3265067 1 6.49
CHEMBL301265 PRAMIPEXOLE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540612 IC50 = 13.0 nM 7.89
CHEMBL3265067 IC50 = 327.0 nM 6.49
CHEMBL301265 PRAMIPEXOLE IC50 - -