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GPCR

NameGlucose-dependent insulinotropic receptor
SpeciesHomo sapiens (Human)
GeneGPR119
SynonymGPCR2
GPR119
G-protein coupled receptor 2
G-protein coupled receptor 119
G protein-coupled receptor 119
[ Show all ]
DiseaseType 2 diabetes
Diabetes
Peripheral arterial disease; Type 2 diabetes
Non-insulin dependent diabetes
Gastric cancer; Type 2 diabetes
Length335
Amino acid sequenceMESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPSRPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLPLGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAGGYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYAYWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG
UniProtQ8TDV5
Protein Data BankN/A
GPCR-HGmod modelQ8TDV5
3D structure modelThis predicted structure model is from GPCR-EXP Q8TDV5.
BioLiPN/A
Therapeutic Target DatabaseT93788
ChEMBLCHEMBL5652
IUPHAR126
DrugBankN/A

Ligand

NameCHEMBL3358004
Molecular formulaC21H23F4N7O3S
IUPAC name[3-fluoro-4-[[2-[(2R)-2-methyl-4-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]piperazin-1-yl]pyrimidin-5-yl]oxymethyl]phenyl]methyl-imino-methyl-oxo-lambda6-sulfane
Molecular weight529.515
Hydrogen bond acceptor14
Hydrogen bond donor1
XlogP3.8
SynonymsBDBM50103553
Inchi KeyCDEAEZQLBRDDDP-OYDRJWEHSA-N
Inchi IDInChI=1S/C21H23F4N7O3S/c1-13-10-31(20-30-29-18(35-20)21(23,24)25)5-6-32(13)19-27-8-16(9-28-19)34-11-15-4-3-14(7-17(15)22)12-36(2,26)33/h3-4,7-9,13,26H,5-6,10-12H2,1-2H3/t13-,36?/m1/s1
PubChem CID118722580
ChEMBLCHEMBL3358004
IUPHARN/A
BindingDB50103553
DrugBankN/A

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand has more than 10 hydrogen bond acceptor.
This ligand is heavier than 500 daltons.

Experimental Data

ParameterValueReferenceDatabase source
EC50158.0 nMPMID25286150BindingDB,ChEMBL
Intrinsic activity101.0 %PMID25286150ChEMBL

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