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Assay Detail

CHEMBL839635

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

Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 3 (CHEMBL2888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
Dominguez C, Prieto L, Valli MJ, Massey SM, Bures M, Wright RA, Johnson BG, Andis SL, Kingston A, Schoepp DD, Monn JA.
J Med Chem (2005) 48 : 3605 -3612
PubMed 15887967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.58 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8759 EGLUMETAD 2.0 1 7.03
CHEMBL192977 1 6.84
CHEMBL192051 2 6.52
CHEMBL365368 1 6.29
CHEMBL195500 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8759 EGLUMETAD Ki = 93.0 nM 7.03
CHEMBL192977 Ki = 146.0 nM 6.84
CHEMBL192051 Ki = 302.0 nM 6.52
CHEMBL365368 Ki = 511.0 nM 6.29
CHEMBL192051 Ki = 570.0 nM 6.24
CHEMBL195500 Ki > 100000.0 nM -