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Assay Detail

CHEMBL1028973

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

Functional
Agonist activity at cyclothiazide-desensitized rat recombinant flop iGluR1 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 1 (CHEMBL3753)
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 4.89 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333964 1 5.55
CHEMBL122005 (S)-WILLARDIINE 1 4.94
CHEMBL337577 1 4.60
CHEMBL121915 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333964 EC50 = 2800.0 nM 5.55
CHEMBL122005 (S)-WILLARDIINE EC50 = 11500.0 nM 4.94
CHEMBL337577 EC50 = 24900.0 nM 4.60
CHEMBL121915 EC50 = 33600.0 nM 4.47