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Assay Detail

CHEMBL715495

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

Binding
Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 4 (CHEMBL2736)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III.
Amori L, Costantino G, Marinozzi M, Pellicciari R, Gasparini F, Flor PJ, Kuhn R, Vranesic I.
Bioorg Med Chem Lett (2000) 10 : 1447 -1450
PubMed 10888329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.24 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33567 1 6.30
CHEMBL34880 1 6.24
CHEMBL284377 DEXFOSFOSERINE 2.0 1 6.00
CHEMBL22136 1 5.36
CHEMBL277475 1 5.33
CHEMBL285043 1 5.16
CHEMBL287703 1 5.10
CHEMBL32142 1 5.05
CHEMBL32976 1 4.57
CHEMBL34453 1 4.41
CHEMBL35111 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33567 EC50 = 500.0 nM 6.30
CHEMBL34880 EC50 = 580.0 nM 6.24
CHEMBL284377 DEXFOSFOSERINE EC50 = 1000.0 nM 6.00
CHEMBL22136 EC50 = 4400.0 nM 5.36
CHEMBL277475 EC50 = 4700.0 nM 5.33
CHEMBL285043 EC50 = 7000.0 nM 5.16
CHEMBL287703 EC50 = 7900.0 nM 5.10
CHEMBL32142 EC50 = 9000.0 nM 5.05
CHEMBL32976 EC50 = 27000.0 nM 4.57
CHEMBL34453 EC50 = 39000.0 nM 4.41
CHEMBL35111 EC50 = 86000.0 nM 4.07