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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

NameCHEMBL1951014
Molecular formulaC21H29N5O5S
IUPAC namepropan-2-yl 4-[5-methyl-6-[(6-methyl-5-methylsulfonylpyridin-2-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate
Molecular weight463.553
Hydrogen bond acceptor9
Hydrogen bond donor1
XlogP2.9
SynonymsBDBM50364544
Inchi KeyVSAANDHHKMNLAM-UHFFFAOYSA-N
Inchi IDInChI=1S/C21H29N5O5S/c1-13(2)30-21(27)26-10-8-16(9-11-26)31-20-14(3)19(22-12-23-20)25-18-7-6-17(15(4)24-18)32(5,28)29/h6-7,12-13,16H,8-11H2,1-5H3,(H,22,23,24,25)
PubChem CID57401105
ChEMBLCHEMBL1951014
IUPHARN/A
BindingDB50364544
DrugBankN/A

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand satisfies Lipinski's rule of five.

Experimental Data

ParameterValueReferenceDatabase source
EC50475.0 nMPMID22264481BindingDB,ChEMBL
Intrinsic activity32.0 %PMID22264481ChEMBL

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