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Assay Detail

CHEMBL4309035

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

Binding
Displacement of [3H]JNJ-46281222 from human mGlu2 receptor expressed in CHOK1 cell membranes preincubated for 3 hrs followed by [3H]JNJ-46281222 addition and measured after 1 hr by microbeta scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 4 7.87 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4589377 1 8.38
CHEMBL4538850 1 8.21
CHEMBL3947764 1 8.12
CHEMBL4468977 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4589377 Ki = 4.169 nM 8.38
CHEMBL4538850 Ki = 6.166 nM 8.21
CHEMBL3947764 Ki = 7.586 nM 8.12
CHEMBL4468977 Ki = 165.96 nM 6.78