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Assay Detail

CHEMBL4027355

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

Binding
Antagonist activity at recombinant rat GluN1a/GluN2A expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method
3
Total Activities
2
Compounds Tested
2
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

Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
Gynther M, Proietti Silvestri I, Hansen JC, Hansen KB, Malm T, Ishchenko Y, Larsen Y, Han L, Kayser S, Auriola S, Petsalo A, Nielsen B, Pickering DS, Bunch L.
J Med Chem (2017) 60 : 9885 -9904
PubMed 29205034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.87 6.41
IC50 1 4.82 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84612 1 6.41
CHEMBL4084540 2 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84612 Ki = 390.0 nM 6.41
CHEMBL4084540 Ki = 4700.0 nM 5.33
CHEMBL4084540 IC50 = 15000.0 nM 4.82