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Assay Detail

CHEMBL3618569

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Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type AV12
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 3 (CHEMBL2888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist.
Monn JA, Prieto L, Taboada L, Hao J, Reinhard MR, Henry SS, Beadle CD, Walton L, Man T, Rudyk H, Clark B, Tupper D, Baker SR, Lamas C, Montero C, Marcos A, Blanco J, Bures M, Clawson DK, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang X, Carter JH, Getman BG, Catlow JT, Swanson S, Johnson BG, Shaw DB, McKinzie DL.
J Med Chem (2015) 58 : 7526 -7548
PubMed 26313429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.63 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.00
CHEMBL3616847 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID EC50 = 1002.0 nM 6.00
CHEMBL3616847 EC50 = 5676.0 nM 5.25