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Assay Detail

CHEMBL747072

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/2AB NMDA expressed in Xenopus oocytes
22
Total Activities
22
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 22 6.88 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117260 1 8.28
CHEMBL19636 1 8.21
CHEMBL19506 1 8.09
CHEMBL116223 1 7.80
CHEMBL419399 1 7.77
CHEMBL325825 1 7.72
CHEMBL326742 1 7.72
CHEMBL326568 1 7.58
CHEMBL325890 1 7.31
CHEMBL117940 1 7.05
CHEMBL116224 1 6.96
CHEMBL113697 1 6.92
CHEMBL115883 1 6.75
CHEMBL114536 1 6.66
CHEMBL324584 1 6.60
CHEMBL114823 1 6.50
CHEMBL114644 1 6.42
CHEMBL115761 1 6.38
CHEMBL324940 1 5.96
CHEMBL113936 1 5.75
CHEMBL113750 1 4.82
CHEMBL114155 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117260 IC50 = 5.3 nM 8.28
CHEMBL19636 IC50 = 6.1 nM 8.21
CHEMBL19506 IC50 = 8.2 nM 8.09
CHEMBL116223 IC50 = 16.0 nM 7.80
CHEMBL419399 IC50 = 17.0 nM 7.77
CHEMBL325825 IC50 = 19.0 nM 7.72
CHEMBL326742 IC50 = 19.0 nM 7.72
CHEMBL326568 IC50 = 26.0 nM 7.58
CHEMBL325890 IC50 = 49.0 nM 7.31
CHEMBL117940 IC50 = 89.0 nM 7.05
CHEMBL116224 IC50 = 110.0 nM 6.96
CHEMBL113697 IC50 = 120.0 nM 6.92
CHEMBL115883 IC50 = 180.0 nM 6.75
CHEMBL114536 IC50 = 220.0 nM 6.66
CHEMBL324584 IC50 = 250.0 nM 6.60
CHEMBL114823 IC50 = 320.0 nM 6.50
CHEMBL114644 IC50 = 380.0 nM 6.42
CHEMBL115761 IC50 = 420.0 nM 6.38
CHEMBL324940 IC50 = 1100.0 nM 5.96
CHEMBL113936 IC50 = 1800.0 nM 5.75
CHEMBL113750 IC50 = 15000.0 nM 4.82
CHEMBL114155 IC50 = 62000.0 nM 4.21