Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL697361

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

Binding
In vitro binding affinity for Ionotropic glutamate receptor AMPA site was determined using [3H]AMPA as radioligand in rat cortex
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

AMPA receptor agonists: synthesis, protolytic properties, and pharmacology of 3-isothiazolol bioisosteres of glutamic acid.
Matzen L, Engesgaard A, Ebert B, Didriksen M, Frølund B, Krogsgaard-Larsen P, Jaroszewski JW.
J Med Chem (1997) 40 : 520 -527
PubMed 9046343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.88 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 7.40
CHEMBL151487 1 6.20
CHEMBL73698 1 6.19
CHEMBL9907 1 5.82
CHEMBL358019 1 5.75
CHEMBL113180 1 5.68
CHEMBL347973 1 5.24
CHEMBL346187 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 40.0 nM 7.40
CHEMBL151487 IC50 = 630.0 nM 6.20
CHEMBL73698 IC50 = 650.0 nM 6.19
CHEMBL9907 IC50 = 1500.0 nM 5.82
CHEMBL358019 IC50 = 1800.0 nM 5.75
CHEMBL113180 IC50 = 2100.0 nM 5.68
CHEMBL347973 IC50 = 5800.0 nM 5.24
CHEMBL346187 IC50 = 17000.0 nM 4.77