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Assay Detail

CHEMBL5579286

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

Binding
Displacement of [3H]-Kainic acid from KA in rat brain membrane preincubated for 15 mins followed by [3H]-Kainic acid addition and measured after 1 hr 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 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 6 6.60 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5589739 1 8.05
CHEMBL5594753 1 7.55
CHEMBL5590005 1 7.55
CHEMBL482097 DOMORIC ACID 1 6.03
CHEMBL5589717 1 5.85
CHEMBL5593727 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5589739 IC50 = 9.0 nM 8.05
CHEMBL5594753 IC50 = 28.0 nM 7.55
CHEMBL5590005 IC50 = 28.0 nM 7.55
CHEMBL482097 DOMORIC ACID IC50 = 940.0 nM 6.03
CHEMBL5589717 IC50 = 1400.0 nM 5.85
CHEMBL5593727 IC50 = 27000.0 nM 4.57