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Assay Detail

CHEMBL866055

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

Binding
Displacement of L[3H]glutamate from GluR in rat brain synaptic membrane
6
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity.
Alonso De Diego SA, Gutiérrez-Rodríguez M, Pérez de Vega MJ, González-Muñiz R, Herranz R, Martín-Martínez M, Cenarruzabeitia E, Frechilla D, Del Río J, Jimeno ML, García-López MT.
Bioorg Med Chem Lett (2006) 16 : 3396 -3400
PubMed 16650992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.38 6.48
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212694 1 6.48
CHEMBL193486 1 5.42
CHEMBL197084 TROFINETIDE 4.0 2 5.10
CHEMBL379934 1 -
CHEMBL211553 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212694 Ki = 330.0 nM 6.48
CHEMBL193486 Ki = 3790.0 nM 5.42
CHEMBL197084 TROFINETIDE Ki = 7960.0 nM 5.10
CHEMBL197084 TROFINETIDE Ki = 31240.0 nM 4.50
CHEMBL379934 Activity - -
CHEMBL211553 Activity - -