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Assay Detail

CHEMBL5579284

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

Binding
Displacement of [3H]-Kainic acid from KA 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 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7.51 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1232313 DOMOIC ACID 1 8.40
CHEMBL275040 KAINIC ACID 2.0 1 7.92
CHEMBL351031 1 7.24
CHEMBL4756304 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1232313 DOMOIC ACID IC50 = 4.0 nM 8.40
CHEMBL275040 KAINIC ACID IC50 = 12.0 nM 7.92
CHEMBL351031 IC50 = 58.0 nM 7.24
CHEMBL4756304 IC50 = 330.0 nM 6.48