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GLASS

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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	CHEMBL2204984
Molecular formula	C23H24N10O
IUPAC name	2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]pyrazole-3-carbonitrile
Molecular weight	456.514
Hydrogen bond acceptor	9
Hydrogen bond donor	0
XlogP	2.7
Synonyms	BDBM50400773 SCHEMBL9883082
Inchi Key	BGLRWXCBFWYRFO-UHFFFAOYSA-N
Inchi ID	InChI=1S/C23H24N10O/c1-2-17-12-25-23(26-13-17)31-9-7-20(8-10-31)33-22(11-24)18(14-28-33)15-34-21-5-3-19(4-6-21)32-16-27-29-30-32/h3-6,12-14,16,20H,2,7-10,15H2,1H3
PubChem CID	67950429
ChEMBL	CHEMBL2204984
IUPHAR	N/A
BindingDB	50400773
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	5.3 nM	PMID24900416	BindingDB
EC50	5.32 nM	PMID24900416	ChEMBL
EC50	10.7 nM	PMID24900416	ChEMBL
EC50	11.0 nM	PMID24900416	BindingDB
Intrinsic activity	76.8 %	PMID24900416	ChEMBL
Intrinsic activity	86.1 %	PMID24900416	ChEMBL
Ki	14.9 nM	PMID24900416	ChEMBL
Ki	15.0 nM	PMID24900416	BindingDB

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