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Assay Detail

CHEMBL934443

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

Binding
Binding affinity at iGluR2o(R) receptor expressed in sf9 cells by radioligand binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor 2 (CHEMBL4016)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.
Beich-Frandsen M, Pickering DS, Mirza O, Johansen TN, Greenwood J, Vestergaard B, Schousboe A, Gajhede M, Liljefors T, Kastrup JS.
J Med Chem (2008) 51 : 1459 -1463
PubMed 18269227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.60 6.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL402444 1 6.63
CHEMBL429594 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL402444 Ki = 234.0 nM 6.63
CHEMBL429594 Ki = 273.0 nM 6.56