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Assay Detail

CHEMBL4371567

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Binding
Agonist activity at human dopamine D2long receptor (unknown origin) expressed in HEK293T cells co-expressing TEV fused-beta-Arrestin2 and GRK2 assessed as increase in beta-arrestin-2 recruitment after overnight incubation by Tango 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

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Tan L, Yan W, McCorvy JD, Cheng J.
J Med Chem (2018) 61 : 9841 -9878
PubMed 29939744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.37 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4467404 1 8.54
CHEMBL4445841 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4467404 EC50 = 2.9 nM 8.54
CHEMBL4445841 EC50 = 6.3 nM 8.20