PPIPT00183

Target Protein Information
Protein_Name C5a anaphylatoxin chemotactic receptor 1
Protein_Sequence MDSFNYTTPDYGHYDDKDTLDLNTPVDKTSNTLRVPDILALVIFAVVFLVGVLGNALVVWVTAFEAKRTINAIWFLNLAVADFLSCLALPILFTSIVQHHHWPFGGAACSILPSLILLNMYASILLLATISADRFLLVFKPIWCQNFRGAGLAWIACAVAWGLALLLTIPSFLYRVVREEYFPPKVLCGVDYSHDKRRERAVAIVRLVLGFLWPLLTLTICYTFILLRTWSRRATRSTKTLKVVVAVVASFFIFWLPYQVTGIMMSFLEPSSPTFLLLKKLDSLCVSFAYINCCINPIIYVVAGQGFQGRLRKSLPSLLRNVLTEESVVRESKSFTRSTVDTMAQKTQAV
Organism_Source Homo sapiens
Functional_Classification G protein-coupled receptor
Cellular_Localization Plasma membrane
Gene_Names C5AR1
UniProt_ID P21730
Protein-Protein Interaction Networks
Peptide Basic Information
Peptide_Name AcF-OPdChaFR (60)
Peptide_Sequence FXPXFWR
Peptide_Length 7
Peptide_SMILES N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)O
Chemical_Modification None
Cyclization_Method Side chain cyclization; Orn2<->Arg6; other bonds
Linear/Cyclic Linear
N-terminal_Modification Acetyl
C-terminal_Modification Free
Amino_Acid_Distribution
Peptide Physicochemical
Molecular_Weight 865.99
Aliphatic_Index 0.00000
Aromaticity 0.42857
Average_Rotatable_Bonds 3.14286
Charge_at_pH_7 0.99798
Isoelectric_point 10.55000
Number_of_Hydrogen_Bond_Acceptors 9
Number_of_Hydrogen_Bond_Donors 11
Topological_Polar_Surface_Area 306.82000
X_logP_energy -0.45123
Interaction Information
Affinity IC50=0.86 uM
Affinity_Assay myeloperoxidase release assay
PDB_ID None
Type Antagonist
Structure
Reference Information
Document_Type Patent
Title CYCLIC PEPTIDES AS G-PROTEIN COUPLED RECEPTOR ANTAGONISTS
Release_Year 2012
Patent_ID US20120302493A1