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Assay Detail

CHEMBL5365007

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

Binding
Antagonist activity at GluN2B receptor (unknown origin) expressed in Xenopus oocytes coexpressing GluN1a at -70 mV holding potential in presence of (S)-glutamate/glycine by TEVC analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2B (CHEMBL1904)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.
Lüken J, Goerges G, Ritter N, Disse P, Schreiber JA, Schmidt J, Frehland B, Schepmann D, Seebohm G, Wünsch B.
J Med Chem (2023) 66 : 11573 -11588
PubMed 37580890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.98 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5435354 1 7.21
CHEMBL5417143 1 7.14
CHEMBL305187 IFENPRODIL 2.0 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5435354 IC50 = 62.0 nM 7.21
CHEMBL5417143 IC50 = 72.0 nM 7.14
CHEMBL305187 IFENPRODIL IC50 = 264.0 nM 6.58