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Assay Detail

CHEMBL1015733

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

Binding
Activity at rat recombinant NR1/NR2C receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology
6
Total Activities
6
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

Glutamate NMDA receptor; Grin1/Grin2c (CHEMBL2096911)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
Clausen RP, Christensen C, Hansen KB, Greenwood JR, Jørgensen L, Micale N, Madsen JC, Nielsen B, Egebjerg J, Bräuner-Osborne H, Traynelis SF, Kristensen JL.
J Med Chem (2008) 51 : 4179 -4187
PubMed 18578474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 4.74 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.00
CHEMBL291278 N-METHYL-D-ASPARTIC ACID (NMDA) 2.0 1 4.64
CHEMBL504772 1 4.27
CHEMBL506027 1 4.04
CHEMBL506409 1 -
CHEMBL453769 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID EC50 = 1000.0 nM 6.00
CHEMBL291278 N-METHYL-D-ASPARTIC ACID (NMDA) EC50 = 23000.0 nM 4.64
CHEMBL504772 EC50 = 54000.0 nM 4.27
CHEMBL506027 EC50 = 91000.0 nM 4.04
CHEMBL506409 EC50 = 255000.0 nM -
CHEMBL453769 EC50 = 429000.0 nM -