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Assay Detail

CHEMBL829838

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

Binding
Displacement of L-[3H]glutamate from N-methyl-D-aspartate glutamate receptor in rat brain synaptic membranes
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure-activity relationships.
Alonso De Diego SA, Muñoz P, González-Muñiz R, Herranz R, Martín-Martínez M, Cenarruzabeitia E, Frechilla D, Del Río J, Jimeno ML, García-López MT.
Bioorg Med Chem Lett (2005) 15 : 2279 -2283
PubMed 15837309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.92 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197208 1 9.00
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.06
CHEMBL193486 1 5.42
CHEMBL84612 1 5.42
CHEMBL197084 TROFINETIDE 4.0 2 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197208 Ki = 1.0 nM 9.00
CHEMBL575060 GLUTAMIC ACID Ki = 870.0 nM 6.06
CHEMBL193486 Ki = 3790.0 nM 5.42
CHEMBL84612 Ki = 3830.0 nM 5.42
CHEMBL197084 TROFINETIDE Ki = 7960.0 nM 5.10
CHEMBL197084 TROFINETIDE Ki = 31240.0 nM 4.50