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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	CHEMBL3354780
Molecular formula	C25H19F4N3O2
IUPAC name	methyl (3R)-3-[(3-fluorophenyl)methyl]-10-[4-(trifluoromethyl)phenyl]-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
Molecular weight	469.44
Hydrogen bond acceptor	8
Hydrogen bond donor	0
XlogP	5.0
Synonyms	BDBM50036643
Inchi Key	ICKZZHZSLWRRAL-XMMPIXPASA-N
Inchi ID	InChI=1S/C25H19F4N3O2/c1-34-23(33)24(12-15-3-2-4-19(26)11-15)10-9-17-13-30-22-20(14-31-32(22)21(17)24)16-5-7-18(8-6-16)25(27,28)29/h2-8,11,13-14H,9-10,12H2,1H3/t24-/m1/s1
PubChem CID	118720408
ChEMBL	CHEMBL3354780
IUPHAR	N/A
BindingDB	50036643
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	3.0 nM	PMID25455488	BindingDB
EC50	3.0 nM	PMID25455488	ChEMBL
Efficacy	92.0 %	PMID25455488	ChEMBL

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