PPIRE05290
Target Protein Information
| Protein_Name | Proteinase-activated receptor 1 |
|---|---|
| Protein_Sequence | MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEEKNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLNIMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTAAFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLKEQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSSAVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVSSISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIYKKLLT |
| Organism_Source | Homo sapiens |
| Functional_Classification | G protein-coupled receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | F2R |
| UniProt_ID | P25116 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | 41 |
|---|---|
| Peptide_Sequence | XXLR |
| Peptide_Length | 4 |
| Peptide_SMILES | CC(C)C[C@H](NC(=O)CNC(=O)CN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O |
| Chemical_Modification | X1=p-fluorophenylalanine; X2=p-guanidinophenylalanine |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Trans-Cinnamoyl |
| C-terminal_Modification | amide |
| Amino_Acid_Distribution | |
|
|
|
Peptide Physicochemical
| Molecular_Weight | 401.47 |
|---|---|
| Aliphatic_Index | 97.50000 |
| Aromaticity | 0.00000 |
| Average_Rotatable_Bonds | 3.25000 |
| Charge_at_pH_7 | 0.99798 |
| Isoelectric_Point | 10.55000 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 6 |
| Number_of_Hydrogen_Bond_Donors | 8 |
| Topological_Polar_Surface_Area | 212.52000 |
| X_logP_energy | -2.57513 |
Interaction Information
| Affinity | IC50=7.8 nM |
|---|---|
| Affinity_Assay | competitive radioligand binding assay |
| 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 |