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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	CHEMBL3358000
Molecular formula	C20H18F4N10O2
IUPAC name	2-[(3R)-4-[5-[[2-fluoro-4-(tetrazol-1-yl)phenyl]methoxy]pyrimidin-2-yl]-3-methylpiperazin-1-yl]-5-(trifluoromethyl)-1,3,4-oxadiazole
Molecular weight	506.426
Hydrogen bond acceptor	15
Hydrogen bond donor	0
XlogP	2.6
Synonyms	BDBM50103557
Inchi Key	AVUCFLHYBFWMSM-GFCCVEGCSA-N
Inchi ID	InChI=1S/C20H18F4N10O2/c1-12-9-32(19-29-28-17(36-19)20(22,23)24)4-5-33(12)18-25-7-15(8-26-18)35-10-13-2-3-14(6-16(13)21)34-11-27-30-31-34/h2-3,6-8,11-12H,4-5,9-10H2,1H3/t12-/m1/s1
PubChem CID	118722576
ChEMBL	CHEMBL3358000
IUPHAR	N/A
BindingDB	50103557
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand has more than 10 hydrogen bond acceptor. This ligand is heavier than 500 daltons.

Experimental Data

Parameter	Value	Reference	Database source
EC50	7.0 nM	PMID25286150	BindingDB
EC50	7.0 nM	PMID25286150	ChEMBL
Intrinsic activity	170.0 %	PMID25286150	ChEMBL

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