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Assay Detail

CHEMBL1029765

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Functional
Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR2(Q) expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor 2 (CHEMBL3503)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.
Butini S, Pickering DS, Morelli E, Coccone SS, Trotta F, De Angelis M, Guarino E, Fiorini I, Campiani G, Novellino E, Schousboe A, Christensen JK, Gemma S.
J Med Chem (2008) 51 : 6614 -6618
PubMed 18811139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.46 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL123132 1 6.34
CHEMBL121388 1 5.68
CHEMBL492630 1 4.93
CHEMBL492469 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL123132 EC50 = 460.0 nM 6.34
CHEMBL121388 EC50 = 2110.0 nM 5.68
CHEMBL492630 EC50 = 11800.0 nM 4.93
CHEMBL492469 EC50 = 12600.0 nM 4.90