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GPCR

NameGlucagon receptor
SpeciesHomo sapiens (Human)
GeneGCGR
SynonymGL-R
GGR
GR
glucagon receptor
DiseaseDiabetes
Type 2 diabetes
Non-insulin dependent diabetes
Obesity; Diabetes
Type 1 diabetes
[ Show all ]
Length477
Amino acid sequenceMPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
UniProtP47871
Protein Data Bank5yqz, 5xez, 5ee7, 5xf1
GPCR-HGmod modelP47871
3D structure modelThis structure is from PDB ID 5yqz.
BioLiPBL0379634,BL0379635, BL0402227, BL0379636,BL0379637, BL0343437
Therapeutic Target DatabaseT60182, T87875
ChEMBLCHEMBL1985
IUPHAR251
DrugBankN/A

Ligand

NameCHEMBL1933365
Molecular formulaC26H27F3N4O3
IUPAC name3-[[4-[cyclopentyl-[[1-[4-(trifluoromethyl)phenyl]pyrazol-4-yl]amino]methyl]benzoyl]amino]propanoic acid
Molecular weight500.522
Hydrogen bond acceptor8
Hydrogen bond donor3
XlogP4.9
SynonymsBDBM50360599
Inchi KeyVERXBCYVZFLZNT-UHFFFAOYSA-N
Inchi IDInChI=1S/C26H27F3N4O3/c27-26(28,29)20-9-11-22(12-10-20)33-16-21(15-31-33)32-24(17-3-1-2-4-17)18-5-7-19(8-6-18)25(36)30-14-13-23(34)35/h5-12,15-17,24,32H,1-4,13-14H2,(H,30,36)(H,34,35)
PubChem CID57393426
ChEMBLCHEMBL1933365
IUPHARN/A
BindingDB50360599
DrugBankN/A

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand is heavier than 500 daltons.

Experimental Data

ParameterValueReferenceDatabase source
Kb120.0 nMPMID22119466ChEMBL
Kb320.0 nMPMID22119466ChEMBL
Ki9.0 nMPMID22119466ChEMBL
Ki17.0 nMPMID22119466BindingDB,ChEMBL

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