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Assay Detail

CHEMBL5041141

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

Binding
Agonist activity at rat GluN1/GluN2B NMDA receptor expressed in Xenopus oocytes measured after 4 days in presence of L-glutamte by two-electrode voltage-clamp recording assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Glutamate NMDA receptor; Grin1/Grin2b (CHEMBL2096666)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Derivatives of (<i>R</i>)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity.
Zhao F, Atxabal U, Mariottini S, Yi F, Lotti JS, Rouzbeh N, Liu N, Bunch L, Hansen KB, Clausen RP.
J Med Chem (2022) 65 : 734 -746
PubMed 34918931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.42 6.62
IC50 2 5.00 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL773 GLYCINE 4.0 1 6.62
CHEMBL285123 (D)-SERINE 3.0 1 6.21
CHEMBL5081008 1 5.00
CHEMBL5090386 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL773 GLYCINE EC50 = 240.0 nM 6.62
CHEMBL285123 (D)-SERINE EC50 = 620.0 nM 6.21
CHEMBL5081008 IC50 = 10000.0 nM 5.00
CHEMBL5090386 IC50 = 10000.0 nM 5.00