PPIPT00857

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-OPdChaWR
Peptide_Sequence AcFXPxWR
Peptide_Length 8
Peptide_SMILES C[C@H](N)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
Chemical_Modification X2=ornithine; X4=cyclohexylalanine
Cyclization_Method Side chain-side chain cyclization; X2<->R6; amide bond
Linear/Cyclic Linear
N-terminal_Modification Acetyl
C-terminal_Modification Amide
Amino_Acid_Distribution
Peptide Physicochemical
Molecular_Weight 893.03
Aliphatic_Index 12.50000
Aromaticity 0.25000
Average_Rotatable_Bonds 2.87500
Charge_at_pH_7 0.93601
Isoelectric_point 8.54991
Number_of_Hydrogen_Bond_Acceptors 11
Number_of_Hydrogen_Bond_Donors 13
Topological_Polar_Surface_Area 335.92000
X_logP_energy -2.25943
Interaction Information
Affinity IC50=0.45 uM
Affinity_Assay radioligand binding assay
PDB_ID None
Type Antagonist
Structure
Reference Information
Document_Type Patent
Title CYCLIC PEPTIDES AS G-PROTEIN-COUPLED RECEPTOR ANTAGONSTS
Release_Year 2006
Patent_ID US20060217530A1