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GLASS

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Go to the GPCR, ligand, or experimental data tables.
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GPCR

Name	Glucose-dependent insulinotropic receptor
Species	Homo sapiens (Human)
Gene	GPR119
Synonym	GPCR2 GPR119 G-protein coupled receptor 2 G-protein coupled receptor 119 G protein-coupled receptor 119 glucose-dependent insulinotropic receptor [ Show all ]
Disease	Type 2 diabetes Diabetes Peripheral arterial disease; Type 2 diabetes Non-insulin dependent diabetes Gastric cancer; Type 2 diabetes
Length	335
Amino acid sequence	MESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPSRPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLPLGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAGGYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYAYWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG
UniProt	Q8TDV5
Protein Data Bank	N/A
GPCR-HGmod model	Q8TDV5
3D structure model	This predicted structure model is from GPCR-EXP Q8TDV5.
BioLiP	N/A
Therapeutic Target Database	T93788
ChEMBL	CHEMBL5652
IUPHAR	126
DrugBank	N/A

Ligand

Name	CHEMBL3326668
Molecular formula	C22H27FN4O6S
IUPAC name	(1-ethylcyclopropyl) 4-[5-fluoro-6-(2-methyl-6-methylsulfonylpyridin-3-yl)oxypyrimidin-4-yl]oxypiperidine-1-carboxylate
Molecular weight	494.538
Hydrogen bond acceptor	10
Hydrogen bond donor	0
XlogP	3.1
Synonyms	BDBM50056005
Inchi Key	QERCQWHYIRCFHH-UHFFFAOYSA-N
Inchi ID	InChI=1S/C22H27FN4O6S/c1-4-22(9-10-22)33-21(28)27-11-7-15(8-12-27)31-19-18(23)20(25-13-24-19)32-16-5-6-17(26-14(16)2)34(3,29)30/h5-6,13,15H,4,7-12H2,1-3H3
PubChem CID	118711776
ChEMBL	CHEMBL3326668
IUPHAR	N/A
BindingDB	50056005
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
EC50	22.0 nM	PMID25088191	BindingDB,ChEMBL
Efficacy	65.0 %	PMID25088191	ChEMBL

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