PPIRE05822
Target Protein Information
| Protein_Name | Proteinase-activated receptor 1 |
|---|---|
| Protein_Sequence | MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEEKNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLNIMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTAAFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLKEQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSSAVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVSSISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIYKKLLT |
| Organism_Source | Homo sapiens |
| Functional_Classification | calcium mobilization |
| Cellular_Localization | Plasma membrane |
| Gene_Names | F2R |
| UniProt_ID | P25116 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | TH146 |
|---|---|
| Peptide_Sequence | rXPGF |
| Peptide_Length | 5 |
| Peptide_SMILES | N=C(N)NCCC[C@H](N)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)O |
| Chemical_Modification | X2=octahydroindole-2-carboxylic acid |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Free |
| C-terminal_Modification | Free |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 532.60 |
|---|---|
| Aliphatic_Index | 0.00000 |
| Aromaticity | 0.20000 |
| Average_Rotatable_Bonds | 2.80000 |
| Charge_at_pH_7 | 0.99798 |
| Isoelectric_Point | 10.55000 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 7 |
| Number_of_Hydrogen_Bond_Donors | 8 |
| Topological_Polar_Surface_Area | 232.83000 |
| X_logP_energy | -2.38753 |
Interaction Information
| Affinity | IC50=110 uM |
|---|---|
| Affinity_Assay | intracellular calcium mobilization assay |
| PDB_ID | None |
| Type | Ion channel modulator |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | The preparation and characterization of novel peptide antagonists to thrombin and factor VIIa and activation of protease-activated receptor 1. |
| Release_Year | 2004 |
| PMID | 15210836 |
| DOI | 10.1124/jpet.104.069229 |