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Assay Detail

CHEMBL4048902

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Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D4 Receptor.
Del Bello F, Bonifazi A, Giorgioni G, Cifani C, Micioni Di Bonaventura MV, Petrelli R, Piergentili A, Fontana S, Mammoli V, Yano H, Matucci R, Vistoli G, Quaglia W.
J Med Chem (2018) 61 : 3712 -3725
PubMed 29589445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pEC50 3 - -
EC50 2 8.86 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4085780 1 9.80
CHEMBL59 DOPAMINE 4.0 1 7.91
CHEMBL3354065 1 -
CHEMBL3354073 1 -
CHEMBL4072818 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4085780 EC50 = 0.1585 nM 9.80
CHEMBL59 DOPAMINE EC50 = 12.3 nM 7.91
CHEMBL3354065 pEC50 - -
CHEMBL3354073 pEC50 - -
CHEMBL4072818 pEC50 - -