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Assay Detail

CHEMBL4394482

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

Binding
Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing Galpahi1/Gbeta1/GFP2-Ggamma2 assessed as Galphai1 dissociation after 15 mins in presence of coelenterazine 400a by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

D<sub>2</sub> Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine.
Shen Y, McCorvy JD, Martini ML, Rodriguiz RM, Pogorelov VM, Ward KM, Wetsel WC, Liu J, Roth BL, Jin J.
J Med Chem (2019) 62 : 4755 -4771
PubMed 30964661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 9.01 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451797 1 9.40
CHEMBL240773 QUINPIROLE 2.0 1 8.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451797 EC50 = 0.4 nM 9.40
CHEMBL240773 QUINPIROLE EC50 = 2.4 nM 8.62