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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

NameCHEMBL442855
Molecular formulaC29H22Cl2N8O2
IUPAC name4-[[3-chloro-4-(4-chlorophenoxy)-N-(6-methyl-1H-benzimidazol-2-yl)anilino]methyl]-N-(2H-tetrazol-5-yl)benzamide
Molecular weight585.449
Hydrogen bond acceptor7
Hydrogen bond donor3
XlogP6.9
Synonyms4-(((3-chloro-4-(4-chlorophenoxy)phenyl)(5-methyl-1H-benzo[d]imidazol-2-yl)amino)methyl)-N-(1H-tetrazol-5-yl)benzamide
BDBM50244079
Inchi KeyAJDHVQNHDFFNGF-UHFFFAOYSA-N
Inchi IDInChI=1S/C29H22Cl2N8O2/c1-17-2-12-24-25(14-17)33-29(32-24)39(16-18-3-5-19(6-4-18)27(40)34-28-35-37-38-36-28)21-9-13-26(23(31)15-21)41-22-10-7-20(30)8-11-22/h2-15H,16H2,1H3,(H,32,33)(H2,34,35,36,37,38,40)
PubChem CID11456034
ChEMBLCHEMBL442855
IUPHARN/A
BindingDB50244079
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
IC50<1000.0 nMPMID18539028BindingDB,ChEMBL
IC5013.0 nMPMID18539028BindingDB,ChEMBL

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