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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

NameCHEMBL2159344
Molecular formulaC33H33Cl2N3O3
IUPAC name3-[[4-[1-[5-(2-cyclohexylphenyl)-3-(3,5-dichlorophenyl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid
Molecular weight590.545
Hydrogen bond acceptor4
Hydrogen bond donor2
XlogP8.1
SynonymsBDBM50393790
Inchi KeyCCXJPCNMWZNEFC-UHFFFAOYSA-N
Inchi IDInChI=1S/C33H33Cl2N3O3/c1-21(22-11-13-24(14-12-22)33(41)36-16-15-32(39)40)38-31(20-30(37-38)25-17-26(34)19-27(35)18-25)29-10-6-5-9-28(29)23-7-3-2-4-8-23/h5-6,9-14,17-21,23H,2-4,7-8,15-16H2,1H3,(H,36,41)(H,39,40)
PubChem CID71454981
ChEMBLCHEMBL2159344
IUPHARN/A
BindingDB50393790
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
IC50337.0 nMPMID22708876BindingDB
IC50337.4 nMPMID22708876ChEMBL
IC50362.0 nMPMID22708876BindingDB,ChEMBL

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