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Assay Detail

CHEMBL1647365

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

Binding
Binding affinity to mGluR1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 1 (CHEMBL3772)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain.
Fujinaga M, Yamasaki T, Kawamura K, Kumata K, Hatori A, Yui J, Yanamoto K, Yoshida Y, Ogawa M, Nengaki N, Maeda J, Fukumura T, Zhang MR.
Bioorg Med Chem (2011) 19 : 102 -110
PubMed 21172734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.93 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL174588 1 9.47
CHEMBL1645349 1 9.40
CHEMBL1645348 1 9.06
CHEMBL1645350 1 8.41
CHEMBL1645351 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL174588 Ki = 0.34 nM 9.47
CHEMBL1645349 Ki = 0.4 nM 9.40
CHEMBL1645348 Ki = 0.87 nM 9.06
CHEMBL1645350 Ki = 3.9 nM 8.41
CHEMBL1645351 Ki = 4.8 nM 8.32