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Assay Detail

CHEMBL5579285

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

Binding
Displacement of [3H]-AMPA from AMPA in rat brain membrane preincubated for 15 mins followed by [3H]-AMPA addition and measured after 40 mins by scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor 4 (CHEMBL3505)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Domoic Acid as a Lead for the Discovery of the First Selective Ligand for Kainate Receptor Subtype 5 (GluK5).
Buschbom-Helmke S, Wang P, Alcaide A, Miguez-Cabello F, Carta M, Viotti JS, Nielsen B, Mulle C, Bowie D, Jørgensen FS, Pickering DS, Bunch L.
J Med Chem (2024) 67 : 14524 -14542
PubMed 39133077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.97 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5589739 1 5.44
CHEMBL5594753 1 5.24
CHEMBL482097 DOMORIC ACID 1 4.92
CHEMBL5590005 1 4.77
CHEMBL5589717 1 4.50
CHEMBL5593727 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5589739 IC50 = 3600.0 nM 5.44
CHEMBL5594753 IC50 = 5700.0 nM 5.24
CHEMBL482097 DOMORIC ACID IC50 = 12000.0 nM 4.92
CHEMBL5590005 IC50 = 17000.0 nM 4.77
CHEMBL5589717 IC50 = 32000.0 nM 4.50
CHEMBL5593727 IC50 > 100000.0 nM -