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Assay Detail

CHEMBL703066

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

Binding
Binding affinity towards Kai-2 using [3]H-kainate as the radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, kainate 5 (CHEMBL2675)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.
Lubisch W, Behl B, Henn C, Hofmann HP, Reeb J, Regner F, Vierling M.
Bioorg Med Chem Lett (2002) 12 : 2113 -2116
PubMed 12127516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 4.96 5.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12465 1 5.01
CHEMBL293613 1 4.96
CHEMBL13076 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12465 Ki = 9800.0 nM 5.01
CHEMBL293613 Ki = 11000.0 nM 4.96
CHEMBL13076 Ki = 12000.0 nM 4.92