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Assay Detail

CHEMBL892223

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

Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assay
5
Total Activities
5
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 Intermediate

Target

Metabotropic glutamate receptor 8 (CHEMBL2718)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.
Marinozzi M, Serpi M, Amori L, Gavilan Diaz M, Costantino G, Meyer U, Flor PJ, Gasparini F, Heckendorn R, Kuhn R, Giorgi G, Hermit MB, Thomsen C, Pellicciari R.
Bioorg Med Chem (2007) 15 : 3161 -3170
PubMed 17350267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.13 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33567 1 5.72
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.47
CHEMBL442076 1 4.20
CHEMBL392420 1 -
CHEMBL396319 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33567 Ki = 1900.0 nM 5.72
CHEMBL575060 GLUTAMIC ACID Ki = 3400.0 nM 5.47
CHEMBL442076 Ki = 63000.0 nM 4.20
CHEMBL392420 Ki = 130000.0 nM -
CHEMBL396319 Ki = 190000.0 nM -