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Assay Detail

CHEMBL901847

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

Functional
Antagonist activity at rat mGlu2 expressed in CHO cells assessed as inhibition of (1S,3R)-ACPD-stimulated GTPgammaS binding
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1.
Woltering TJ, Adam G, Alanine A, Wichmann J, Knoflach F, Mutel V, Gatti S.
Bioorg Med Chem Lett (2007) 17 : 6811 -6815
PubMed 17964783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.87 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304285 1 5.22
CHEMBL290509 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304285 IC50 = 6000.0 nM 5.22
CHEMBL290509 IC50 = 30000.0 nM 4.52