Assay Detail

CHEMBL4719944

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Binding

Agonist activity at mGlu3 (unknown origin)

ChEMBL ↗

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Target

Metabotropic glutamate receptor 3 (CHEMBL2888) ↗

Open DB target context

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Metabotropic glutamate receptor 3 (CHEMBL2888) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Metabotropic glutamate receptor 3

CHEMBL2888

Anchored from Assay target.

Protein identity Metabotropic glutamate receptor 3

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Metabotropic glutamate receptor 3 (CHEMBL2888) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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	3	7.90	8.20

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2381643	—	—	1	8.20
CHEMBL2381642	—	—	1	7.95
CHEMBL8759	EGLUMETAD	2.0	1	7.55

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2381643	—	IC50	=	6.3	nM	8.20
CHEMBL2381642	—	IC50	=	11.2	nM	7.95
CHEMBL8759	EGLUMETAD	IC50	=	27.9	nM	7.55