Assay Detail

CHEMBL680013

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

Binding

Ability to displace [3H]LY-341,495 binding to Group II Metabotropic glutamate receptor from rat forebrain

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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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
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors.

Monn JA, Valli MJ, Massey SM, Hansen MM, Kress TJ, Wepsiec JP, Harkness AR, Grutsch JL, Wright RA, Johnson BG, Andis SL, Kingston A, Tomlinson R, Lewis R, Griffey KR, Tizzano JP, Schoepp DD.
J Med Chem (1999) 42 : 1027 -1040
PubMed 10090786 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	7	7.00	8.08

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL8839	LY-389795	—	3	8.08
CHEMBL275079	LY-379268	—	3	7.82
CHEMBL8759	EGLUMETAD	2.0	1	6.59

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL8839	LY-389795	IC50	=	8.4	nM	8.08
CHEMBL275079	LY-379268	IC50	=	15.0	nM	7.82
CHEMBL8839	LY-389795	IC50	=	26.1	nM	7.58
CHEMBL275079	LY-379268	IC50	=	29.0	nM	7.54
CHEMBL8759	EGLUMETAD	IC50	=	254.0	nM	6.59
CHEMBL8839	LY-389795	IC50	=	792.0	nM	6.10
CHEMBL275079	LY-379268	IC50	=	5040.0	nM	5.30