PPIRE07658
Target Protein Information
| Protein_Name | Gastrin-releasing peptide receptor |
|---|---|
| Protein_Sequence | MDPNNCSHLNLEVDPFLSCNNTFNQTLNPPKMDNWFHPGIIYVIPAVYGLIIVIGLIGNITLIKIFCTVKSMRNVPNLFISSLALGDLLLLVTCAPVDASKYLADRWLFGRIGCKLIPFIQLTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAALIWIVSMLLAIPEAVFSDLHPFHVKDTNQTFISCAPYPHSNELHPKIHSMASFLVFYIIPLSIISVYYYFIARNLIQSAYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFITSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPSLLNRSHSTGRSTTCMTSFKSTNPSATFSLINGNICHEGYV |
| Organism_Source | Rattus norvegicus |
| Functional_Classification | G protein-coupled receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | Grpr |
| UniProt_ID | P52500 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | Peptide 18 |
|---|---|
| Peptide_Sequence | fQWAVGHL |
| Peptide_Length | 8 |
| Peptide_SMILES | CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)C(=O)O |
| Chemical_Modification | None |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Acetyl |
| C-terminal_Modification | CH2NHCOCH3 |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 957.10 |
|---|---|
| Aliphatic_Index | 97.50000 |
| Aromaticity | 0.25000 |
| Average_Rotatable_Bonds | 3.37500 |
| Charge_at_pH_7 | 0.08889 |
| Isoelectric_Point | 7.55032 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 11 |
| Number_of_Hydrogen_Bond_Donors | 12 |
| Topological_Polar_Surface_Area | 354.58000 |
| X_logP_energy | -0.65670 |
Interaction Information
| Affinity | IC50=55 nM |
|---|---|
| Affinity_Assay | Enzyme Inhibition Kinetics |
| PDB_ID | None |
| Type | antagonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Identification of novel classes of protein kinase inhibitors using combinatorial peptide chemistry based on functional genomics knowledge. |
| Release_Year | 1992 |
| PMID | 10072688 |
| DOI | 10.1021/jm980573a |