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Assay Detail

CHEMBL4408256

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

Binding
Positive allosteric modulation of recombinant rat GluN1/GluN2A receptor expressed in Xenopus laevis oocytes assessed as increase in glycine/L-glutamate-induced channel current at -80 mV holding potential by two-electrode voltage clamp method
1
Total Activities
1
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

Neuroactive Steroid <i>N</i>-Methyl-d-aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity.
La DS, Salituro FG, Martinez Botella G, Griffin AM, Bai Z, Ackley MA, Dai J, Doherty JJ, Harrison BL, Hoffmann EC, Kazdoba TM, Lewis MC, Quirk MC, Robichaud AJ.
J Med Chem (2019) 62 : 7526 -7542
PubMed 31390523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.19 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL171804 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL171804 EC50 = 650.0 nM 6.19