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GPCR

NameGastric inhibitory polypeptide receptor
SpeciesHomo sapiens (Human)
GeneGIPR
SynonymGIP-R
GIP receptor
Glucose-dependent insulinotropic polypeptide receptor
Gippr
DiseaseType 2 diabetes
Length466
Amino acid sequenceMTTSPILQLLLRLSLCGLLLQRAETGSKGQTAGELYQRWERYRRECQETLAAAEPPSGLACNGSFDMYVCWDYAAPNATARASCPWYLPWHHHVAAGFVLRQCGSDGQWGLWRDHTQCENPEKNEAFLDQRLILERLQVMYTVGYSLSLATLLLALLILSLFRRLHCTRNYIHINLFTSFMLRAAAILSRDRLLPRPGPYLGDQALALWNQALAACRTAQIVTQYCVGANYTWLLVEGVYLHSLLVLVGGSEEGHFRYYLLLGWGAPALFVIPWVIVRYLYENTQCWERNEVKAIWWIIRTPILMTILINFLIFIRILGILLSKLRTRQMRCRDYRLRLARSTLTLVPLLGVHEVVFAPVTEEQARGALRFAKLGFEIFLSSFQGFLVSVLYCFINKEVQSEIRRGWHHCRLRRSLGEEQRQLPERAFRALPSGSGPGEVPTSRGLSSGTLPGPGNEASRELESYC
UniProtP48546
Protein Data BankN/A
GPCR-HGmod modelP48546
3D structure modelThis predicted structure model is from GPCR-EXP P48546.
BioLiPN/A
Therapeutic Target DatabaseT41750
ChEMBLCHEMBL4383
IUPHAR248
DrugBankN/A

Ligand

Namethiazole, 30
Molecular formulaC29H22F6N2O5S
IUPAC name(2R)-2-hydroxy-3-[[4-[2-[4-(trifluoromethoxy)phenyl]-2-[4-[4-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]ethyl]benzoyl]amino]propanoic acid
Molecular weight624.554
Hydrogen bond acceptor13
Hydrogen bond donor3
XlogP6.6
SynonymsCHEMBL501392
BDBM29133
Inchi KeyNGUABMKOSJANPJ-SYIFMXBLSA-N
Inchi IDInChI=1S/C29H22F6N2O5S/c30-28(31,32)20-9-5-18(6-10-20)23-15-43-26(37-23)22(17-7-11-21(12-8-17)42-29(33,34)35)13-16-1-3-19(4-2-16)25(39)36-14-24(38)27(40)41/h1-12,15,22,24,38H,13-14H2,(H,36,39)(H,40,41)/t22?,24-/m1/s1
PubChem CID42617999
ChEMBLCHEMBL501392
IUPHARN/A
BindingDB29133
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.
This ligand has a partition coefficient log P greater than 5.

Experimental Data

ParameterValueReferenceDatabase source
IC50565.0 nMPMID19385613BindingDB,ChEMBL

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