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Assay Detail

CHEMBL4040529

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

Binding
Positive allosteric modulation of human metabotropic glutamate receptor 2 expressed in CHOK1 cells assessed as cellular impedance measured for 20 mins with 15 sec time interval followed by 40 mins with 5 mins time interval and subsequently measured with 15 mins time interval in presence of endogenous glutamate levels by RTCA
3
Total Activities
3
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

Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2.
Doornbos MLJ, Cid JM, Haubrich J, Nunes A, van de Sande JW, Vermond SC, Mulder-Krieger T, Trabanco AA, Ahnaou A, Drinkenburg WH, Lavreysen H, Heitman LH, IJzerman AP, Tresadern G.
J Med Chem (2017) 60 : 6704 -6720
PubMed 28704052 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.58 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4063313 1 7.95
CHEMBL4064589 1 7.73
CHEMBL4067290 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4063313 EC50 = 11.22 nM 7.95
CHEMBL4064589 EC50 = 18.62 nM 7.73
CHEMBL4067290 EC50 = 89.13 nM 7.05