PPIRE02516
Target Protein Information
| Protein_Name | Proteinase-activated receptor 1 |
|---|---|
| Protein_Sequence | MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEEKNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLNIMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTAAFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLKEQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSSAVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVSSISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIYKKLLT |
| Organism_Source | Homo sapiens |
| Functional_Classification | Receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | F2R |
| UniProt_ID | P25116 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | BMS-200261 |
|---|---|
| Peptide_Sequence | XXLRR |
| Peptide_Length | 5 |
| Peptide_SMILES | CC(C)C[C@H](NC(=O)CNC(=O)CN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O |
| Chemical_Modification | X1=p-fluoroPhe; X2=p-guanidinoPhe |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Other |
| C-terminal_Modification | amide |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 557.65 |
|---|---|
| Aliphatic_Index | 78.00000 |
| Aromaticity | 0.00000 |
| Average_Rotatable_Bonds | 3.80000 |
| Charge_at_pH_7 | 1.99798 |
| Isoelectric_Point | 12.50011 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 8 |
| Number_of_Hydrogen_Bond_Donors | 12 |
| Topological_Polar_Surface_Area | 303.52000 |
| X_logP_energy | -3.82706 |
Interaction Information
| Affinity | IC50=16.6 nM |
|---|---|
| Affinity_Assay | NMR chemical shift perturbation |
| PDB_ID | None |
| Type | antagonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Development of potent thrombin receptor antagonist peptides. |
| Release_Year | 1996 |
| PMID | 8960546 |
| DOI | 10.1021/jm960455s |