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GPCR

NameFree fatty acid receptor 1
SpeciesHomo sapiens (Human)
GeneFFAR1
SynonymFFA1R
G protein-coupled receptor 40
G-protein coupled receptor 40
GPR40
FFA1 receptor
DiseaseType 2 diabetes
Non-insulin dependent diabetes
Diabetes
Length300
Amino acid sequenceMDLPPQLSFGLYVAAFALGFPLNVLAIRGATAHARLRLTPSLVYALNLGCSDLLLTVSLPLKAVEALASGAWPLPASLCPVFAVAHFFPLYAGGGFLAALSAGRYLGAAFPLGYQAFRRPCYSWGVCAAIWALVLCHLGLVFGLEAPGGWLDHSNTSLGINTPVNGSPVCLEAWDPASAGPARFSLSLLLFFLPLAITAFCYVGCLRALARSGLTHRRKLRAAWVAGGALLTLLLCVGPYNASNVASFLYPNLGGSWRKLGLITGAWSVVLNPLVTGYLGRGPGLKTVCAARTQGGKSQK
UniProtO14842
Protein Data Bank5tzy, 5tzr
GPCR-HGmod modelO14842
3D structure modelThis structure is from PDB ID 5tzy.
BioLiPBL0380462, BL0380463, BL0380464
Therapeutic Target DatabaseT25608
ChEMBLCHEMBL4422
IUPHAR225
DrugBankBE0000688

Ligand

NameCHEMBL2151293
Molecular formulaC27H29FO4
IUPAC name3-[3-[[3-tert-butyl-4-(2-fluoro-5-methoxyphenyl)phenyl]methoxy]phenyl]propanoic acid
Molecular weight436.523
Hydrogen bond acceptor5
Hydrogen bond donor1
XlogP6.5
SynonymsBDBM50392874
SCHEMBL2503614
Inchi KeyBJOXXURHNRXMAX-UHFFFAOYSA-N
Inchi IDInChI=1S/C27H29FO4/c1-27(2,3)24-15-19(8-11-22(24)23-16-20(31-4)10-12-25(23)28)17-32-21-7-5-6-18(14-21)9-13-26(29)30/h5-8,10-12,14-16H,9,13,17H2,1-4H3,(H,29,30)
PubChem CID57705863
ChEMBLCHEMBL2151293
IUPHARN/A
BindingDB50392874
DrugBankN/A

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand has a partition coefficient log P greater than 5.

Experimental Data

ParameterValueReferenceDatabase source
EC50900.0 nMPMID24900539BindingDB,ChEMBL
Efficacy113.0 %PMID24900539ChEMBL

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