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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

NameCHEMBL2159341
Molecular formulaC32H27Cl2N3O3
IUPAC name3-[[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methylnaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid
Molecular weight572.486
Hydrogen bond acceptor4
Hydrogen bond donor2
XlogP7.2
SynonymsBDBM50393785
Inchi KeyKNTOEHKTBLUGLN-FQEVSTJZSA-N
Inchi IDInChI=1S/C32H27Cl2N3O3/c1-19-3-4-24-14-25(10-9-23(24)13-19)30-18-29(26-15-27(33)17-28(34)16-26)36-37(30)20(2)21-5-7-22(8-6-21)32(40)35-12-11-31(38)39/h3-10,13-18,20H,11-12H2,1-2H3,(H,35,40)(H,38,39)/t20-/m0/s1
PubChem CID60170856
ChEMBLCHEMBL2159341
IUPHARN/A
BindingDB50393785
DrugBankN/A

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand is heavier than 500 daltons.
This ligand has a partition coefficient log P greater than 5.

Experimental Data

ParameterValueReferenceDatabase source
IC50753.0 nMPMID22708876BindingDB,ChEMBL

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