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Assay Detail

CHEMBL834064

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

Functional
In vitro activity at Ionotropic glutamate receptor using cortical wedge assays in rat brain synaptosoma
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, kainate 3 (CHEMBL3744)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.
Vogensen SB, Clausen RP, Greenwood JR, Johansen TN, Pickering DS, Nielsen B, Ebert B, Krogsgaard-Larsen P.
J Med Chem (2005) 48 : 3438 -3442
PubMed 15857151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.50 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370038 1 6.96
CHEMBL94859 1 6.48
CHEMBL370941 1 5.46
CHEMBL276815 (S)-AMPA 1 5.42
CHEMBL372643 1 4.50
CHEMBL193087 1 4.15
CHEMBL317790 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370038 EC50 = 110.0 nM 6.96
CHEMBL94859 EC50 = 330.0 nM 6.48
CHEMBL370941 EC50 = 3500.0 nM 5.46
CHEMBL276815 (S)-AMPA EC50 = 3800.0 nM 5.42
CHEMBL372643 EC50 = 32000.0 nM 4.50
CHEMBL193087 EC50 = 71000.0 nM 4.15
CHEMBL317790 EC50 > 1000000.0 nM -