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Assay Detail

CHEMBL4719931

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

Binding
Antagonist activity at human recombinant mGlu7 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type AV12
Subcellular Cell membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
Chappell MD,Li R,Smith SC,Dressman BA,Tromiczak EG,Tripp AE,Blanco MJ,Vetman T,Quimby SJ,Matt J,Britton TC,Fivush AM,Schkeryantz JM,Mayhugh D,Erickson JA,Bures MG,Jaramillo C,Carpintero M,Diego JE,Barberis M,Garcia-Cerrada S,Soriano JF,Antonysamy S,Atwell S,MacEwan I,Condon B,Sougias C,Wang J,Zhang A,Conners K,Groshong C,Wasserman SR,Koss JW,Witkin JM,Li X,Overshiner C,Wafford KA,Seidel W,Wang XS,Heinz BA,Swanson S,Catlow JT,Bedwell DW,Monn JA,Mitch CH,Ornstein PL
J Med Chem (2016) 59 : 10974 -10993
PubMed 28002967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.90 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4751065 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4751065 IC50 = 1260.0 nM 5.90