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Assay Detail

CHEMBL4194320

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

Binding
Modulation of recombinant human GluN1/GluN2B NMDA receptor expressed in mammalian cells assessed as inhibition of glutamate/glycine-induced intracellular calcium flux pretreated for 5 mins followed by glutamate/glycine addition measured after 5 mins by calcium 5 dye based FLIPR assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Modulating GluN2B for the Treatment of Neurological and Psychiatric Disorders.
Kargbo RB.
ACS Med Chem Lett (2017) 8 : 905 -907
PubMed 28947933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205952 1 8.70
CHEMBL4211247 1 8.20
CHEMBL4217661 1 8.00
CHEMBL4206361 1 7.90
CHEMBL4214203 1 7.80
CHEMBL4202517 1 7.70
CHEMBL4210730 1 7.70
CHEMBL4206877 1 7.60
CHEMBL4215686 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205952 IC50 = 1.995 nM 8.70
CHEMBL4211247 IC50 = 6.31 nM 8.20
CHEMBL4217661 IC50 = 10.0 nM 8.00
CHEMBL4206361 IC50 = 12.59 nM 7.90
CHEMBL4214203 IC50 = 15.85 nM 7.80
CHEMBL4202517 IC50 = 19.95 nM 7.70
CHEMBL4210730 IC50 = 19.95 nM 7.70
CHEMBL4206877 IC50 = 25.12 nM 7.60
CHEMBL4215686 IC50 = 50.12 nM 7.30