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Assay Detail

CHEMBL718350

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

Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RGT
Confidence 9 — Direct 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. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability.
Ornstein PL, Bleisch TJ, Arnold MB, Kennedy JH, Wright RA, Johnson BG, Tizzano JP, Helton DR, Kallman MJ, Schoepp DD, Hérin M.
J Med Chem (1998) 41 : 358 -378
PubMed 9464367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.82 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432038 1 8.00
CHEMBL124501 1 7.10
CHEMBL2112634 1 7.10
CHEMBL341457 1 6.80
CHEMBL124078 1 6.77
CHEMBL333771 1 6.75
CHEMBL2111822 1 6.75
CHEMBL123842 1 6.70
CHEMBL338282 1 6.68
CHEMBL124483 1 6.58
CHEMBL123847 1 6.38
CHEMBL2112582 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432038 IC50 = 10.0 nM 8.00
CHEMBL124501 IC50 = 80.0 nM 7.10
CHEMBL2112634 IC50 = 80.0 nM 7.10
CHEMBL341457 IC50 = 160.0 nM 6.80
CHEMBL124078 IC50 = 170.0 nM 6.77
CHEMBL333771 IC50 = 180.0 nM 6.75
CHEMBL2111822 IC50 = 180.0 nM 6.75
CHEMBL123842 IC50 = 200.0 nM 6.70
CHEMBL338282 IC50 = 210.0 nM 6.68
CHEMBL124483 IC50 = 260.0 nM 6.58
CHEMBL123847 IC50 = 420.0 nM 6.38
CHEMBL2112582 IC50 = 650.0 nM 6.19