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Assay Detail

CHEMBL747078

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

Functional
Tested for the NMDA antagonist activity using a functional assay, by protection of cultured hippocampus neurons from the toxic effects of extracellularly applied glutamate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2C (CHEMBL401)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Oxindole N-Methyl-D-Aspartate (NMDA) antagonists
Chenard B, Butler T, Shalaby I, Prochniak M, Koe B, Fox C
Bioorg Med Chem Lett (1993) 3 : 91 -94
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.72 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366809 1 7.40
CHEMBL319706 (S)-IFENPRODIL 1 7.26
CHEMBL427116 1 6.96
CHEMBL172807 1 6.64
CHEMBL49623 (R,S)-IFENPRODIL 1 6.58
CHEMBL173092 1 6.22
CHEMBL28564 ELIPRODIL 2.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366809 IC50 = 40.0 nM 7.40
CHEMBL319706 (S)-IFENPRODIL IC50 = 55.0 nM 7.26
CHEMBL427116 IC50 = 111.0 nM 6.96
CHEMBL172807 IC50 = 231.0 nM 6.64
CHEMBL49623 (R,S)-IFENPRODIL IC50 = 263.0 nM 6.58
CHEMBL173092 IC50 = 600.0 nM 6.22
CHEMBL28564 ELIPRODIL IC50 = 1000.0 nM 6.00