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Assay Detail

CHEMBL4309033

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

Functional
Positive allosteric modulation of human mGlu2 receptor expressed in CHOK1 cell membranes assessed as increase in glutamate-induced [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins by scintillation spectrometry method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization.
Doornbos MLJ, Wang X, Vermond SC, Peeters L, Pérez-Benito L, Trabanco AA, Lavreysen H, Cid JM, Heitman LH, Tresadern G, IJzerman AP.
J Med Chem (2018) 62 : 223 -233
PubMed 29494768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.29 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4589377 1 7.82
CHEMBL3947764 1 7.74
CHEMBL4468977 1 6.80
CHEMBL4538850 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4589377 EC50 = 15.14 nM 7.82
CHEMBL3947764 EC50 = 18.2 nM 7.74
CHEMBL4468977 EC50 = 158.49 nM 6.80
CHEMBL4538850 EC50 = 158.49 nM 6.80