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Assay Detail

CHEMBL747069

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

Binding
Concentration required for 50% Inhibition of responses at cloned NR1A/2A NMDA expressed in Xenopus oocytes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Oocyte
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL2015)
Type SINGLE PROTEIN
Organism Homo sapiens

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 19 4.30 4.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116223 1 4.60
CHEMBL117260 1 4.46
CHEMBL19506 1 4.42
CHEMBL113697 1 4.41
CHEMBL117940 1 4.41
CHEMBL114823 1 4.28
CHEMBL113936 1 4.24
CHEMBL115883 1 4.12
CHEMBL114155 1 4.05
CHEMBL324584 1 4.02
CHEMBL326568 1 -
CHEMBL115761 1 -
CHEMBL116224 1 -
CHEMBL113750 1 -
CHEMBL326742 1 -
CHEMBL324940 1 -
CHEMBL19636 1 -
CHEMBL114644 1 -
CHEMBL114536 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116223 IC50 = 25000.0 nM 4.60
CHEMBL117260 IC50 = 35000.0 nM 4.46
CHEMBL19506 IC50 = 38000.0 nM 4.42
CHEMBL113697 IC50 = 39000.0 nM 4.41
CHEMBL117940 IC50 = 39000.0 nM 4.41
CHEMBL114823 IC50 = 52000.0 nM 4.28
CHEMBL113936 IC50 = 57000.0 nM 4.24
CHEMBL115883 IC50 = 75000.0 nM 4.12
CHEMBL114155 IC50 = 89000.0 nM 4.05
CHEMBL324584 IC50 = 95000.0 nM 4.02
CHEMBL326568 IC50 > 100000.0 nM -
CHEMBL115761 IC50 > 100000.0 nM -
CHEMBL116224 IC50 > 100000.0 nM -
CHEMBL113750 IC50 > 100000.0 nM -
CHEMBL326742 IC50 > 100000.0 nM -
CHEMBL324940 IC50 > 100000.0 nM -
CHEMBL19636 IC50 > 100000.0 nM -
CHEMBL114644 IC50 > 100000.0 nM -
CHEMBL114536 IC50 > 100000.0 nM -