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Assay Detail

CHEMBL2168914

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

Functional
Partial agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists.
Chen X, Sassano MF, Zheng L, Setola V, Chen M, Bai X, Frye SV, Wetsel WC, Roth BL, Jin J.
J Med Chem (2012) 55 : 7141 -7153
PubMed 22845053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.60 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160296 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160296 EC50 = 2.5 nM 8.60