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Assay Detail

CHEMBL718205

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

Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 2 expressed in RGT cells.
22
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 2 (CHEMBL5137)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid.
Valli MJ, Schoepp DD, Wright RA, Johnson BG, Kingston AE, Tomlinson R, Monn JA.
Bioorg Med Chem Lett (1998) 8 : 1985 -1990
PubMed 9873471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.36 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302411 1 4.70
CHEMBL293434 2 4.44
CHEMBL304919 1 4.43
CHEMBL60164 1 4.38
CHEMBL418650 1 4.33
CHEMBL61281 1 4.30
CHEMBL39338 1 4.30
CHEMBL292553 1 4.21
CHEMBL418462 1 4.12
CHEMBL59830 1 -
CHEMBL300330 1 -
CHEMBL60008 1 -
CHEMBL59920 1 -
CHEMBL58247 1 -
CHEMBL61964 1 -
CHEMBL1169414 1 -
CHEMBL304034 1 -
CHEMBL406215 1 -
CHEMBL60238 2 -
CHEMBL60302 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302411 IC50 = 20000.0 nM 4.70
CHEMBL293434 IC50 = 36000.0 nM 4.44
CHEMBL304919 IC50 = 37300.0 nM 4.43
CHEMBL60164 IC50 = 42000.0 nM 4.38
CHEMBL418650 IC50 = 46200.0 nM 4.33
CHEMBL61281 IC50 = 50000.0 nM 4.30
CHEMBL39338 IC50 = 50000.0 nM 4.30
CHEMBL292553 IC50 = 61000.0 nM 4.21
CHEMBL418462 IC50 = 75000.0 nM 4.12
CHEMBL59830 IC50 > 300000.0 nM -
CHEMBL293434 IC50 > 300000.0 nM -
CHEMBL300330 IC50 > 300000.0 nM -
CHEMBL60008 IC50 > 300000.0 nM -
CHEMBL59920 IC50 > 300000.0 nM -
CHEMBL60238 IC50 > 300000.0 nM -
CHEMBL58247 IC50 = 339000.0 nM -
CHEMBL61964 IC50 > 300000.0 nM -
CHEMBL1169414 IC50 > 300000.0 nM -
CHEMBL304034 IC50 > 300000.0 nM -
CHEMBL406215 IC50 > 300000.0 nM -
CHEMBL60238 IC50 = 121000.0 nM -
CHEMBL60302 IC50 > 300000.0 nM -