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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

NameCHEMBL3326671
Molecular formulaC21H22F4N4O7S
IUPAC name[3-(trifluoromethyl)oxetan-3-yl] 4-[5-fluoro-6-(2-methyl-6-methylsulfonylpyridin-3-yl)oxypyrimidin-4-yl]oxypiperidine-1-carboxylate
Molecular weight550.482
Hydrogen bond acceptor14
Hydrogen bond donor0
XlogP2.5
SynonymsBDBM50056008
Inchi KeyPMXJGYIIFVVUMX-UHFFFAOYSA-N
Inchi IDInChI=1S/C21H22F4N4O7S/c1-12-14(3-4-15(28-12)37(2,31)32)35-18-16(22)17(26-11-27-18)34-13-5-7-29(8-6-13)19(30)36-20(9-33-10-20)21(23,24)25/h3-4,11,13H,5-10H2,1-2H3
PubChem CID118711779
ChEMBLCHEMBL3326671
IUPHARN/A
BindingDB50056008
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
EC5029.0 nMPMID25088191BindingDB
EC5029.3 nMPMID25088191ChEMBL
Efficacy66.0 %PMID25088191ChEMBL

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