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Assay Detail

CHEMBL4394479

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

Binding
Antagonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as inhibition of dopamine-stimulated beta-arrestin2 recruitment measured after 20 to 22 hrs by brightglo-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
IC50 2 7.00 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451797 1 7.15
CHEMBL42 CLOZAPINE 4.0 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451797 IC50 = 71.0 nM 7.15
CHEMBL42 CLOZAPINE IC50 = 140.0 nM 6.85