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Assay Detail

CHEMBL828680

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

Binding
Inhibitory concentration against human recombinant metabotropic glutamate receptor 5 (mGlu5) in Ltk cells determined using fluorescence detection method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Ltk
Confidence 9 — Direct single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 5 (CHEMBL3227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Bonnefous C, Vernier JM, Hutchinson JH, Chung J, Reyes-Manalo G, Kamenecka T.
Bioorg Med Chem Lett (2005) 15 : 1197 -1200
PubMed 15686941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.22 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361973 1 8.30
CHEMBL292065 1 8.30
CHEMBL180964 1 8.15
CHEMBL180713 1 8.10
CHEMBL361556 1 7.96
CHEMBL181769 1 7.96
CHEMBL182762 1 7.92
CHEMBL181332 1 7.68
CHEMBL181424 1 7.66
CHEMBL181169 1 7.64
CHEMBL183081 1 7.55
CHEMBL441117 1 7.50
CHEMBL359893 1 6.99
CHEMBL178854 1 6.98
CHEMBL178328 1 6.87
CHEMBL179387 1 6.84
CHEMBL367145 1 6.80
CHEMBL178683 1 6.78
CHEMBL178841 1 6.59
CHEMBL361116 1 5.45
CHEMBL181610 1 5.42
CHEMBL178530 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361973 IC50 = 5.0 nM 8.30
CHEMBL292065 IC50 = 5.0 nM 8.30
CHEMBL180964 IC50 = 7.0 nM 8.15
CHEMBL180713 IC50 = 8.0 nM 8.10
CHEMBL361556 IC50 = 11.0 nM 7.96
CHEMBL181769 IC50 = 11.0 nM 7.96
CHEMBL182762 IC50 = 12.0 nM 7.92
CHEMBL181332 IC50 = 21.0 nM 7.68
CHEMBL181424 IC50 = 22.0 nM 7.66
CHEMBL181169 IC50 = 23.0 nM 7.64
CHEMBL183081 IC50 = 28.0 nM 7.55
CHEMBL441117 IC50 = 32.0 nM 7.50
CHEMBL359893 IC50 = 103.0 nM 6.99
CHEMBL178854 IC50 = 105.0 nM 6.98
CHEMBL178328 IC50 = 134.0 nM 6.87
CHEMBL179387 IC50 = 145.0 nM 6.84
CHEMBL367145 IC50 = 158.0 nM 6.80
CHEMBL178683 IC50 = 165.0 nM 6.78
CHEMBL178841 IC50 = 254.0 nM 6.59
CHEMBL361116 IC50 = 3536.0 nM 5.45
CHEMBL181610 IC50 = 3800.0 nM 5.42
CHEMBL178530 IC50 = 5084.0 nM 5.29