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Assay Detail

CHEMBL1817061

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Functional
Agonist activity at non-desensitized homomeric rat GluK3 mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
Venskutonyte R, Butini S, Coccone SS, Gemma S, Brindisi M, Kumar V, Guarino E, Maramai S, Valenti S, Amir A, Valadés EA, Frydenvang K, Kastrup JS, Novellino E, Campiani G, Pickering DS.
J Med Chem (2011) 54 : 4793 -4805
PubMed 21619066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 4.35 4.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288166 2S,4R-4-METHYLGLUTAMATE 1 4.35
CHEMBL575060 GLUTAMIC ACID 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288166 2S,4R-4-METHYLGLUTAMATE EC50 = 45100.0 nM 4.35
CHEMBL575060 GLUTAMIC ACID EC50 = 9030000.0 nM -