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Assay Detail

CHEMBL699701

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

Binding
Ability to inhibit [3H]-KA binding to Ionotropic glutamate receptor kainate from rat cortical membranes.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, kainate (CHEMBL2094119)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis, resolution, and biological evaluation of the four stereoisomers of 4-methylglutamic acid: selective probes of kainate receptors.
Gu ZQ, Hesson DP, Pelletier JC, Maccecchini ML, Zhou LM, Skolnick P.
J Med Chem (1995) 38 : 2518 -2520
PubMed 7629789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.10 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275040 KAINIC ACID 2.0 1 7.96
CHEMBL288166 2S,4R-4-METHYLGLUTAMATE 1 7.46
CHEMBL85447 1 7.09
CHEMBL41221 1 6.51
CHEMBL289439 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275040 KAINIC ACID IC50 = 11.0 nM 7.96
CHEMBL288166 2S,4R-4-METHYLGLUTAMATE IC50 = 35.0 nM 7.46
CHEMBL85447 IC50 = 82.0 nM 7.09
CHEMBL41221 IC50 = 310.0 nM 6.51
CHEMBL289439 IC50 = 330.0 nM 6.48