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Assay Detail

CHEMBL3876535

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

Binding
Displacement of [3H]-JNJ-40068782 from human mGlu2 receptor expressed in HEK293 cell membranes coexpressing rat glutamate transporter measured after 30 mins in presence of orthosteric antagonist LY341495 by liquid scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 2 (CHEMBL5137)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia.
Higgins MA, Marcin LR, Christopher Zusi F, Gentles R, Ding M, Pearce BC, Easton A, Kostich WA, Seager MA, Bourin C, Bristow LJ, Johnson KA, Miller R, Hogan J, Whiterock V, Gulianello M, Ferrante M, Huang Y, Hendricson A, Alt A, Macor JE, Bronson JJ.
Bioorg Med Chem (2017) 25 : 496 -513
PubMed 27914948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3885379 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3885379 Ki = 1.0 nM 9.00