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GPCR

NameGlucose-dependent insulinotropic receptor
SpeciesRattus norvegicus (Rat)
GeneGpr119
SynonymG protein-coupled receptor 119
G-protein coupled receptor 119
G-protein coupled receptor 2
glucose-dependent insulinotropic receptor
GPCR2
[ Show all ]
DiseaseN/A for non-human GPCRs
Length468
Amino acid sequenceMESSFSFGVILAVLTILIIAVNALVVVAMLLSIYKNDGVGLCFTLNLAVADTLIGVAISGLVTDQLSSSAQHTQKTLCSLRMAFVTSSAAASVLTVMLIAFDRYLAIKQPLRYFQIMNGLVAGGCIAGLWLISYLIGFLPLGVSIFQQTTYHGPCTFFAVFHPRFVLTLSCAGFFPAVLLFVFFYCDMLKIASVHSQHIRKMEHAGAMVGACRPPRPVNDFKAVRTVSVLIGSFTLSWSPFLITSIVQVACHKCCLYQVLEKYLWLLGVGNSLLNPLIYAYWQREVRQQLCHMALGLLADGSTQPQIETLKGKEERKKVGRKTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDACDTQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDTQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDAQTLYTSSLVTGQTEQTPLKRANMSDPLRTCRG
UniProtQ7TQN8
Protein Data BankN/A
GPCR-HGmod modelN/A
3D structure modelNo available structures or models
BioLiPN/A
Therapeutic Target DatabaseN/A
ChEMBLCHEMBL5262
IUPHARN/A
DrugBankN/A

Ligand

NameAPD597
Molecular formulaC21H29N5O6S
IUPAC namepropan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate
Molecular weight479.552
Hydrogen bond acceptor10
Hydrogen bond donor1
XlogP2.5
SynonymsMolPort-042-665-884
BCP17733
EX-A1213
isopropyl 4-((5-methoxy-6-((2-methyl-6-(methylsulfonyl)pyridin-3-yl)amino)pyrimidin-4-yl)oxy)piperidine-1-carboxylate
SB16860
[ Show all ]
Inchi KeyWPDCHTSXOPUOII-UHFFFAOYSA-N
Inchi IDInChI=1S/C21H29N5O6S/c1-13(2)31-21(27)26-10-8-15(9-11-26)32-20-18(30-4)19(22-12-23-20)25-16-6-7-17(24-14(16)3)33(5,28)29/h6-7,12-13,15H,8-11H2,1-5H3,(H,22,23,25)
PubChem CID11691484
ChEMBLCHEMBL1951032
IUPHAR5727
BindingDB50364559
DrugBankN/A

Structure

SDF download

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

Experimental Data

ParameterValueReferenceDatabase source
EC50421.0 nMPMID26048791, PMID25088191, PMID22264481BindingDB,ChEMBL
Efficacy89.0 %PMID25088191ChEMBL
Emax89.0 %PMID26048791ChEMBL
Intrinsic activity89.0 %PMID22264481ChEMBL

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