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Assay Detail

CHEMBL718352

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

Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 3 (CHEMBL2888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution.
Ornstein PL, Bleisch TJ, Arnold MB, Wright RA, Johnson BG, Schoepp DD.
J Med Chem (1998) 41 : 346 -357
PubMed 9464366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.18 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL144151 1 7.80
CHEMBL2311086 1 6.55
CHEMBL2112583 1 6.33
CHEMBL2112584 1 6.26
CHEMBL2112581 1 6.24
CHEMBL2112582 1 6.19
CHEMBL2112586 1 6.12
CHEMBL2112580 1 5.92
CHEMBL2112574 1 5.85
CHEMBL331753 1 5.75
CHEMBL2112579 1 5.60
CHEMBL2112585 1 5.55
CHEMBL333487 1 -
CHEMBL332141 1 -
CHEMBL325500 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL144151 IC50 = 16.0 nM 7.80
CHEMBL2311086 IC50 = 280.0 nM 6.55
CHEMBL2112583 IC50 = 470.0 nM 6.33
CHEMBL2112584 IC50 = 550.0 nM 6.26
CHEMBL2112581 IC50 = 570.0 nM 6.24
CHEMBL2112582 IC50 = 650.0 nM 6.19
CHEMBL2112586 IC50 = 760.0 nM 6.12
CHEMBL2112580 IC50 = 1200.0 nM 5.92
CHEMBL2112574 IC50 = 1400.0 nM 5.85
CHEMBL331753 IC50 = 1800.0 nM 5.75
CHEMBL2112579 IC50 = 2500.0 nM 5.60
CHEMBL2112585 IC50 = 2800.0 nM 5.55
CHEMBL333487 IC50 > 10000.0 nM -
CHEMBL332141 IC50 > 10000.0 nM -
CHEMBL325500 IC50 > 10000.0 nM -