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Assay Detail

CHEMBL749986

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

Functional
Functional NMDA receptor antagonism expressed as inhibition of NMDA/glycine induced increase in cytosolic calcium in cultured rat cerebellar granule cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis, biological activity, and absolute stereochemical assignment of NPS 1392: a potent and stereoselective NMDA receptor antagonist.
Moe ST, Shimizu SM, Smith DL, Van Wagenen BC, DelMar EG, Balandrin MF, Chien Y, Raszkiewicz JL, Artman LD, Mueller AL, Lobkovsky E, Clardy J.
Bioorg Med Chem Lett (1999) 9 : 1915 -1920
PubMed 10450953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.30 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284237 DIZOCILPINE 2.0 1 8.47
CHEMBL294852 1 7.20
CHEMBL293092 1 7.12
CHEMBL59371 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284237 DIZOCILPINE IC50 = 3.4 nM 8.47
CHEMBL294852 IC50 = 63.0 nM 7.20
CHEMBL293092 IC50 = 75.0 nM 7.12
CHEMBL59371 IC50 = 384.0 nM 6.42