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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	CHEMBL3354804
Molecular formula	C26H22F4N4O
IUPAC name	[(3R)-3-cyclopropyl-3-[(3-fluorophenyl)methyl]-10-[4-(trifluoromethyl)phenyl]-1,4,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraen-11-yl]methanol
Molecular weight	482.483
Hydrogen bond acceptor	8
Hydrogen bond donor	2
XlogP	3.6
Synonyms	BDBM50036671
Inchi Key	GLSPPSAFNUHLJA-RUZDIDTESA-N
Inchi ID	InChI=1S/C26H22F4N4O/c27-20-3-1-2-15(10-20)11-25(18-8-9-18)23-17(13-32-25)12-31-24-22(21(14-35)33-34(23)24)16-4-6-19(7-5-16)26(28,29)30/h1-7,10,12,18,32,35H,8-9,11,13-14H2/t25-/m1/s1
PubChem CID	118720431
ChEMBL	CHEMBL3354804
IUPHAR	N/A
BindingDB	50036671
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	2.0 nM	PMID25455488	BindingDB
EC50	2.0 nM	PMID25455488	ChEMBL
Efficacy	88.0 %	PMID25455488	ChEMBL

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