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Assay Detail

CHEMBL752244

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

Binding
In vitro inhibition of NMDA responses at NR1A/2B receptor expressed in Xenopus oocytes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, NMDA 3A (CHEMBL342)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Subtype-selective N-methyl-D-aspartate receptor antagonists: benzimidazalone and hydantoin as phenol replacements.
Schelkun RM, Yuen PW, Serpa K, Meltzer LT, Wise LD, Whittemore ER, Woodward RM.
J Med Chem (2000) 43 : 1892 -1897
PubMed 10794706 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.74 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54778 1 7.60
CHEMBL56643 1 7.02
CHEMBL293491 1 6.96
CHEMBL56702 1 5.47
CHEMBL58826 1 5.00
CHEMBL58992 1 4.96
CHEMBL56155 1 4.57
CHEMBL442165 1 4.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54778 IC50 = 25.0 nM 7.60
CHEMBL56643 IC50 = 95.0 nM 7.02
CHEMBL293491 IC50 = 110.0 nM 6.96
CHEMBL56702 IC50 = 3400.0 nM 5.47
CHEMBL58826 IC50 = 10000.0 nM 5.00
CHEMBL58992 IC50 = 11000.0 nM 4.96
CHEMBL56155 IC50 = 27000.0 nM 4.57
CHEMBL442165 IC50 = 49000.0 nM 4.31