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Assay Detail

CHEMBL802683

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

Functional
Antagonistic activity was evaluated by using ACPD sensitive [3H]-glutamate binding assay in rat forebrain membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Forebrain
Subcellular Membrane
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors.
Collado I, Ezquerra J, Mazón A, Pedregal C, Yruretagoyena B, Kingston AE, Tomlinson R, Wright RA, Johnson BG, Schoepp DD.
Bioorg Med Chem Lett (1998) 8 : 2849 -2854
PubMed 9873635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.60 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432038 1 8.00
CHEMBL329920 1 7.30
CHEMBL97574 1 7.15
CHEMBL316521 1 6.28
CHEMBL329953 1 5.59
CHEMBL95444 1 5.29
CHEMBL100208 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432038 IC50 = 10.0 nM 8.00
CHEMBL329920 IC50 = 50.0 nM 7.30
CHEMBL97574 IC50 = 71.0 nM 7.15
CHEMBL316521 IC50 = 530.0 nM 6.28
CHEMBL329953 IC50 = 2540.0 nM 5.59
CHEMBL95444 IC50 = 5070.0 nM 5.29
CHEMBL100208 IC50 > 10000.0 nM -