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Assay Detail

CHEMBL5041143

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

Binding
Agonist activity at rat GluN1/GluN2D NMDA receptor expressed in Xenopus oocytes measured after 4 days in presence of L-glutamte by two-electrode voltage-clamp recording assay
12
Total Activities
12
Compounds Tested
1
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

Ionotropic glutamate receptor NMDA 1/2D (CHEMBL3038506)
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 12 6.11 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5081078 1 7.10
CHEMBL773 GLYCINE 4.0 1 7.04
CHEMBL5081008 1 6.82
CHEMBL285123 (D)-SERINE 3.0 1 6.82
CHEMBL5091289 1 6.64
CHEMBL5085583 1 6.58
CHEMBL5081203 1 6.57
CHEMBL5087170 1 5.50
CHEMBL5072895 1 5.37
CHEMBL5076681 1 5.30
CHEMBL5087550 1 5.11
CHEMBL5083882 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5081078 EC50 = 80.0 nM 7.10
CHEMBL773 GLYCINE EC50 = 91.0 nM 7.04
CHEMBL5081008 EC50 = 150.0 nM 6.82
CHEMBL285123 (D)-SERINE EC50 = 150.0 nM 6.82
CHEMBL5091289 EC50 = 230.0 nM 6.64
CHEMBL5085583 EC50 = 260.0 nM 6.58
CHEMBL5081203 EC50 = 270.0 nM 6.57
CHEMBL5087170 EC50 = 3200.0 nM 5.50
CHEMBL5072895 EC50 = 4300.0 nM 5.37
CHEMBL5076681 EC50 = 5000.0 nM 5.30
CHEMBL5087550 EC50 = 7700.0 nM 5.11
CHEMBL5083882 EC50 = 31000.0 nM 4.51