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Assay Detail

CHEMBL4254527

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

Binding
Antagonist activity at GluN2B/GluN1a receptor (unknown origin) expressed in mouse L(tk-) cells assessed as cytoprotection against glycine/(S)-glutamate-induced cell death preincubated for 30 mins followed by glycine/(S)-glutamate addition measured after 6 hrs by LDH assay
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.
Temme L, Frehland B, Schepmann D, Robaa D, Sippl W, Wünsch B.
Eur J Med Chem (2018) 144 : 672 -681
PubMed 29289890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.88 7.75
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305195 1 7.75
CHEMBL305187 IFENPRODIL 2.0 1 6.23
CHEMBL4284348 1 5.52
CHEMBL4294991 2 5.28
CHEMBL4286654 1 4.60
CHEMBL4287755 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305195 IC50 = 18.0 nM 7.75
CHEMBL305187 IFENPRODIL IC50 = 590.0 nM 6.23
CHEMBL4284348 IC50 = 3000.0 nM 5.52
CHEMBL4294991 IC50 = 5200.0 nM 5.28
CHEMBL4286654 IC50 = 25000.0 nM 4.60
CHEMBL4287755 IC50 > 100000.0 nM -
CHEMBL4294991 Inhibition - % -