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Assay Detail

CHEMBL4423745

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

Binding
Positive allosteric modulation of rat GluN1/GluN2A expressed in Xenopus laevis oocytes assessed as potentiation of L-glutamate/glycine-induced current response at holding potential -60 mV by two-electrode voltage clamp method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate NMDA receptor; Grin1/Grin2a (CHEMBL2096680)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Investigation of the structural requirements for N-methyl-D-aspartate receptor positive and negative allosteric modulators based on 2-naphthoic acid.
Irvine MW, Fang G, Sapkota K, Burnell ES, Volianskis A, Costa BM, Culley G, Collingridge GL, Monaghan DT, Jane DE.
Eur J Med Chem (2019) 164 : 471 -498
PubMed 30622023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 4.66 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4530995 1 5.12
CHEMBL4467653 1 4.57
CHEMBL4452216 1 4.55
CHEMBL4531020 1 4.41
CHEMBL4572997 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4530995 EC50 = 7500.0 nM 5.12
CHEMBL4467653 EC50 = 26700.0 nM 4.57
CHEMBL4452216 EC50 = 28000.0 nM 4.55
CHEMBL4531020 EC50 = 39400.0 nM 4.41
CHEMBL4572997 EC50 = 114400.0 nM -