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Assay Detail

CHEMBL2182829

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Functional
Antagonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHOp
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.
Spetea M, Berzetei-Gurske IP, Guerrieri E, Schmidhammer H.
J Med Chem (2012) 55 : 10302 -10306
PubMed 23134120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.84 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180641 1 5.90
CHEMBL2180639 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180641 IC50 = 1252.0 nM 5.90
CHEMBL2180639 IC50 = 1647.0 nM 5.78