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Assay Detail

CHEMBL5579283

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

Binding
Displacement of [3H]-AMPA from AMPA in rat synaptic membrane
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Synaptosome
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 4 6.54 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4756304 1 7.22
CHEMBL351031 1 6.89
CHEMBL1232313 DOMOIC ACID 1 6.33
CHEMBL275040 KAINIC ACID 2.0 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4756304 IC50 = 60.0 nM 7.22
CHEMBL351031 IC50 = 130.0 nM 6.89
CHEMBL1232313 DOMOIC ACID IC50 = 470.0 nM 6.33
CHEMBL275040 KAINIC ACID IC50 = 1900.0 nM 5.72