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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

NameCHEMBL197851
Molecular formulaC28H32F3N7O3
IUPAC name4-[[8-tert-butyl-2-oxo-3-[4-(trifluoromethoxy)phenyl]-1,3-diazaspiro[4.5]decan-1-yl]methyl]-N-(2H-tetrazol-5-yl)benzamide
Molecular weight571.605
Hydrogen bond acceptor9
Hydrogen bond donor2
XlogP5.5
SynonymsSCHEMBL5946488
BDBM50171836
SCHEMBL2665894
4-[8-tert-Butyl-2-oxo-3-(4-trifluoromethoxy-phenyl)-1,3-diaza-spiro[4.5]dec-1-ylmethyl]-N-(1H-tetrazol-5-yl)-benzamide
Inchi KeyBTHIALRARVMMLP-UHFFFAOYSA-N
Inchi IDInChI=1S/C28H32F3N7O3/c1-26(2,3)20-12-14-27(15-13-20)17-37(21-8-10-22(11-9-21)41-28(29,30)31)25(40)38(27)16-18-4-6-19(7-5-18)23(39)32-24-33-35-36-34-24/h4-11,20H,12-17H2,1-3H3,(H2,32,33,34,35,36,39)
PubChem CID10370821
ChEMBLCHEMBL197851
IUPHARN/A
BindingDB50171836
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
IC50105.0 nMPMID16102966BindingDB,ChEMBL
IC50193.0 nMPMID16102966BindingDB,ChEMBL

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