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Assay Detail

CHEMBL981463

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

Functional
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modulations of the amide function of the preferential dopamine D3 agonist (R,R)-S32504: improvements of affinity and selectivity for D3 versus D2 receptors.
Peglion JL, Poitevin C, Mannoury La Cour C, Dupuis D, Millan MJ.
Bioorg Med Chem Lett (2009) 19 : 2133 -2138
PubMed 19324548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.62 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484598 1 8.85
CHEMBL484599 1 8.64
CHEMBL485128 1 8.64
CHEMBL484732 1 8.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484598 EC50 = 1.413 nM 8.85
CHEMBL484599 EC50 = 2.291 nM 8.64
CHEMBL485128 EC50 = 2.291 nM 8.64
CHEMBL484732 EC50 = 4.677 nM 8.33