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Assay Detail

CHEMBL1639366

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

Binding
Displacement of [3H]LY354740 from recombinant rat mGluR2 expressed in CHO cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 2 (CHEMBL2851)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
Woltering TJ, Wichmann J, Goetschi E, Knoflach F, Ballard TM, Huwyler J, Gatti S.
Bioorg Med Chem Lett (2010) 20 : 6969 -6974
PubMed 20971004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.01 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261288 1 7.80
CHEMBL411440 1 7.58
CHEMBL401446 1 7.47
CHEMBL394287 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261288 IC50 = 16.0 nM 7.80
CHEMBL411440 IC50 = 26.0 nM 7.58
CHEMBL401446 IC50 = 34.0 nM 7.47
CHEMBL394287 IC50 = 6400.0 nM 5.19