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Assay Detail

CHEMBL2328014

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Functional
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucose-dependent insulinotropic receptor (CHEMBL5652)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 5-nitropyrimidine analogs with azabicyclic substituents as GPR119 agonists.
Yang Z, Fang Y, Pham TA, Lee J, Park H.
Bioorg Med Chem Lett (2013) 23 : 1519 -1521
PubMed 23374864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.05 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084479 2 8.85
CHEMBL3084483 1 8.82
CHEMBL3084480 2 8.31
CHEMBL3084481 1 8.17
CHEMBL3084484 1 7.94
CHEMBL280065 OLEOYLETHANOLAMIDE 1 5.66
CHEMBL3084482 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084479 EC50 = 1.4 nM 8.85
CHEMBL3084479 EC50 = 1.5 nM 8.82
CHEMBL3084483 EC50 = 1.5 nM 8.82
CHEMBL3084480 EC50 = 4.9 nM 8.31
CHEMBL3084481 EC50 = 6.7 nM 8.17
CHEMBL3084484 EC50 = 11.5 nM 7.94
CHEMBL3084480 EC50 = 14.5 nM 7.84
CHEMBL280065 OLEOYLETHANOLAMIDE EC50 = 2200.0 nM 5.66
CHEMBL3084482 EC50 > 10000.0 nM -