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Assay Detail

CHEMBL751793

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

Binding
The compound was tested in vitro for the inhibition of N-methyl-D-aspartate glutamate receptor in rat cerebellar granule cells (RCGCs).
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Chiral synthesis and pharmacological evaluation of NPS 1407: a potent, stereoselective NMDA receptor antagonist.
Moe ST, Smith DL, DelMar EG, Shimizu SM, Van Wagenen BC, Balandrin MF, Chien YE, Raszkiewicz JL, Artman LD, White HS, Mueller AL.
Bioorg Med Chem Lett (2000) 10 : 2411 -2415
PubMed 11078190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.11 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
CHEMBL78767 1 7.05
CHEMBL421144 1 6.84
CHEMBL79133 1 5.96

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
CHEMBL78767 IC50 = 89.0 nM 7.05
CHEMBL421144 IC50 = 145.0 nM 6.84
CHEMBL79133 IC50 = 1110.0 nM 5.96