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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	APD597
Molecular formula	C21H29N5O6S
IUPAC name	propan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate
Molecular weight	479.552
Hydrogen bond acceptor	10
Hydrogen bond donor	1
XlogP	2.5
Synonyms	BCP17733 EX-A1213 MolPort-042-665-884 AKOS026751481 CHEMBL1951032 isopropyl 4-((5-methoxy-6-((2-methyl-6-(methylsulfonyl)pyridin-3-yl)amino)pyrimidin-4-yl)oxy)piperidine-1-carboxylate SB16860 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester DB12084 JNJ38431055 WPDCHTSXOPUOII-UHFFFAOYSA-N 897732-93-3 BDBM50364559 GTPL5727 propan-2-yl 4-({6-[(6-methanesulfonyl-2-methylpyridin-3-yl)amino]-5-methoxypyrimidin-4-yl}oxy)piperidine-1-carboxylate APD 597 CS-5278 JNJ 38431055 SCHEMBL386884 APD597(JNJ-38431055) DTXSID10237885 KB-146004 ZINC38256220 ADP-597 HY-15566 propan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate 345354O7AT APD-597 D0O9XN JNJ-38431055 UNII-345354O7AT [ Show all ]
Inchi Key	WPDCHTSXOPUOII-UHFFFAOYSA-N
Inchi ID	InChI=1S/C21H29N5O6S/c1-13(2)31-21(27)26-10-8-15(9-11-26)32-20-18(30-4)19(22-12-23-20)25-16-6-7-17(24-14(16)3)33(5,28)29/h6-7,12-13,15H,8-11H2,1-5H3,(H,22,23,25)
PubChem CID	11691484
ChEMBL	CHEMBL1951032
IUPHAR	5727
BindingDB	50364559
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	46.0 nM	PMID26048791, PMID25088191, PMID22264481	BindingDB,ChEMBL
EC50	50.1187 nM	PMID22264481	IUPHAR
Efficacy	75.0 %	PMID25088191	ChEMBL
Emax	75.0 %	PMID26048791	ChEMBL
Intrinsic activity	75.0 %	PMID22264481	ChEMBL

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