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Assay Detail

CHEMBL3294082

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Functional
Positive allosteric modulation of rat mGluR2 receptor expressed in HEK293A cells by calcium mobilization assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293-A
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.
Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND.
J Med Chem (2014) 57 : 4154 -4172
PubMed 24735492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.14 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287695 1 7.92
CHEMBL593013 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287695 EC50 = 12.0 nM 7.92
CHEMBL593013 EC50 = 441.0 nM 6.36