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Assay Detail

CHEMBL709764

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

Binding
In vitro ability to displace [3H]glutamate binding to metabotropic glutamate receptors in rat forebrain membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: identification of a potent, highly selective, and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase.
Monn JA, Valli MJ, Johnson BG, Salhoff CR, Wright RA, Howe T, Bond A, Lodge D, Spangle LA, Paschal JW, Campbell JB, Griffey K, Tizzano JP, Schoepp DD.
J Med Chem (1996) 39 : 2990 -3000
PubMed 8709133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.09 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40086 1 5.19
CHEMBL34453 1 4.99
CHEMBL323097 1 -
CHEMBL103452 1 -
CHEMBL431998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40086 IC50 = 6490.0 nM 5.19
CHEMBL34453 IC50 = 10300.0 nM 4.99
CHEMBL323097 IC50 > 100000.0 nM -
CHEMBL103452 IC50 > 100000.0 nM -
CHEMBL431998 IC50 > 100000.0 nM -