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Assay Detail

CHEMBL5136765

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

Binding
Positive allosteric modulation of recombinant human GluN1/GluN2C receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by whole cell patch clamp method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Ionotropic glutamate receptor NMDA 1/2C (CHEMBL3038504)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

SAGE-718: A First-in-Class <i>N</i>-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment.
Hill MD, Blanco MJ, Salituro FG, Bai Z, Beckley JT, Ackley MA, Dai J, Doherty JJ, Harrison BL, Hoffmann EC, Kazdoba TM, Lanzetta D, Lewis M, Quirk MC, Robichaud AJ.
J Med Chem (2022) 65 : 9063 -9075
PubMed 35785990 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.82 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5095095 DALZANEMDOR 3.0 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5095095 DALZANEMDOR EC50 = 150.0 nM 6.82