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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	CHEMBL2010853
Molecular formula	C23H25F2N3O3S2
IUPAC name	N-[(3S,4R)-3-fluoro-1-[(5-fluoro-1,3-benzothiazol-2-yl)methyl]piperidin-4-yl]-N-methyl-2-(4-methylsulfonylphenyl)acetamide
Molecular weight	493.588
Hydrogen bond acceptor	8
Hydrogen bond donor	0
XlogP	3.3
Synonyms	BDBM50379159
Inchi Key	BKCLNIGTOQSNPO-AZUAARDMSA-N
Inchi ID	InChI=1S/C23H25F2N3O3S2/c1-27(23(29)11-15-3-6-17(7-4-15)33(2,30)31)20-9-10-28(13-18(20)25)14-22-26-19-12-16(24)5-8-21(19)32-22/h3-8,12,18,20H,9-11,13-14H2,1-2H3/t18-,20+/m0/s1
PubChem CID	70687332
ChEMBL	CHEMBL2010853
IUPHAR	N/A
BindingDB	50379159
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Activity	39.0 %	PMID22061639	ChEMBL
EC50	18.0 nM	PMID22061639	BindingDB,ChEMBL

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