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Assay Detail

CHEMBL3869614

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

Binding
Displacement of [3H]-LY459477 from human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing human EAAT1 after 90 mins by liquid scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.
Dressman BA, Tromiczak EG, Chappell MD, Tripp AE, Quimby SJ, Vetman T, Fivush AM, Matt J, Jaramillo C, Li R, Khilevich A, Blanco MJ, Smith SC, Carpintero M, de Diego JE, Barberis M, García-Cerrada S, Soriano JF, Schkeryantz JM, Witkin JM, Wafford KA, Seidel W, Britton T, Overshiner CD, Li X, Wang XS, Heinz BA, Catlow JT, Swanson S, Bedwell D, Ornstein PL, Mitch CH.
Bioorg Med Chem Lett (2016) 26 : 5663 -5668
PubMed 27836401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.57 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3969063 1 8.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3969063 Ki = 2.7 nM 8.57