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Assay Detail

CHEMBL863305

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

Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type BHK
Confidence 9 — Direct single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 4 (CHEMBL2787)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.
Amori L, Serpi M, Marinozzi M, Costantino G, Diaz MG, Hermit MB, Thomsen C, Pellicciari R.
Bioorg Med Chem Lett (2006) 16 : 196 -199
PubMed 16213710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.42 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33567 1 6.80
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.47
CHEMBL197976 1 5.13
CHEMBL199626 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33567 Ki = 160.0 nM 6.80
CHEMBL575060 GLUTAMIC ACID Ki = 3400.0 nM 5.47
CHEMBL197976 Ki = 7400.0 nM 5.13
CHEMBL199626 Ki = 53000.0 nM 4.28