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Assay Detail

CHEMBL671404

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

Binding
Displacement of [3H]raclopride at Dopamine receptor D2 in brain striata (n=1)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines.
Wright JL, Gregory TF, Kesten SR, Boxer PA, Serpa KA, Meltzer LT, Wise LD, Espitia SA, Konkoy CS, Whittemore ER, Woodward RM.
J Med Chem (2000) 43 : 3408 -3419
PubMed 10978188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.06 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19506 1 5.77
CHEMBL117260 1 5.58
CHEMBL325825 1 5.43
CHEMBL19636 1 5.41
CHEMBL326568 1 5.00
CHEMBL419399 1 4.85
CHEMBL19576 1 4.39
CHEMBL326742 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19506 IC50 = 1700.0 nM 5.77
CHEMBL117260 IC50 = 2600.0 nM 5.58
CHEMBL325825 IC50 = 3700.0 nM 5.43
CHEMBL19636 IC50 = 3900.0 nM 5.41
CHEMBL326568 IC50 = 9900.0 nM 5.00
CHEMBL419399 IC50 = 14000.0 nM 4.85
CHEMBL19576 IC50 = 41000.0 nM 4.39
CHEMBL326742 IC50 = 86000.0 nM 4.07