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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

NameCHEMBL3325851
Molecular formulaC20H24F2N4O6S
IUPAC name[(2S)-1-fluoropropan-2-yl] 4-[5-fluoro-6-(2-methyl-6-methylsulfonylpyridin-3-yl)oxypyrimidin-4-yl]oxypiperidine-1-carboxylate
Molecular weight486.491
Hydrogen bond acceptor11
Hydrogen bond donor0
XlogP2.6
SynonymsBDBM50056001
Inchi KeyBKEOSKPDNQWDSX-LBPRGKRZSA-N
Inchi IDInChI=1S/C20H24F2N4O6S/c1-12(10-21)30-20(27)26-8-6-14(7-9-26)31-18-17(22)19(24-11-23-18)32-15-4-5-16(25-13(15)2)33(3,28)29/h4-5,11-12,14H,6-10H2,1-3H3/t12-/m0/s1
PubChem CID118711218
ChEMBLCHEMBL3325851
IUPHARN/A
BindingDB50056001
DrugBankN/A

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand has more than 10 hydrogen bond acceptor.

Experimental Data

ParameterValueReferenceDatabase source
EC50186.0 nMPMID25088191BindingDB,ChEMBL
Efficacy72.0 %PMID25088191ChEMBL

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