Assay Detail

CHEMBL680166

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Binding

Inhibitory concentration against ACPD-sensitive radioligand [3H]glutamate binding to Group II Metabotropic glutamate receptor in rat forebrain membranes

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

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
Tissue	Forebrain
Subcellular	Membrane
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties.

Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL, Griffey KR, Tizzano JP, Kallman MJ, Helton DR, Schoepp DD.
J Med Chem (1997) 40 : 528 -537
PubMed 9046344 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	5	6.53	6.75

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL8759	EGLUMETAD	2.0	3	6.75
CHEMBL280563	—	—	1	6.34
CHEMBL358200	—	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL8759	EGLUMETAD	IC50	=	180.0	nM	6.75
CHEMBL8759	EGLUMETAD	IC50	=	318.0	nM	6.50
CHEMBL280563	—	IC50	=	454.0	nM	6.34
CHEMBL358200	—	IC50	>	100000.0	nM	-
CHEMBL8759	EGLUMETAD	IC50	>	100000.0	nM	-