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Target
Gastrin-releasing peptide receptor
Ligand
BDBM50040321
Substrate
n/a
Meas. Tech.
ChEMBL_458 (CHEMBL615688)
IC50
7.3±n/a nM
Citation
 Leban, JJ; Landavazo, A; McDermed, JD; Diliberto, EJ; Jansen, M; Stockstill, B; Kull, FC Potent gastrin-releasing peptide (GRP) antagonists derived from GRP (19-27) with a C-terminal DPro psi [CH2NH]Phe-NH2 and N-terminal aromatic residues. J Med Chem 37:439-45 (1994) [PubMed]
Target
Name:
Gastrin-releasing peptide receptor
Synonyms:
GRP-R | GRP-preferring bombesin receptor | GRPR_MOUSE | Gastrin releasing peptide receptor | Gastrin-releasing peptide receptor | Grpr
Type:
Enzyme Catalytic Domain
Mol. Mass.:
43234.59
Organism:
MOUSE
Description:
Gastrin-Releasing peptide 0 MOUSE::P21729
Residue:
384
Sequence:
MAPNNCSHLNLDVDPFLSCNDTFNQSLSPPKMDNWFHPGFIYVIPAVYGLIIVIGLIGNITLIKIFCTVKSMRNVPNLFISSLALGDLLLLVTCAPVDASKYLADRWLFGRIGCKLIPFIQLTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAALIWIVSMLLAIPEAVFSDLHPFHVKDTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLAIISVYYYFIARNLIQSAYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLMNRSHSTGRSTTCMTSFKSTNPSATFSLINRNICHEGYV
  
Inhibitor
Name:
BDBM50040321
Synonyms:
CHEMBL385805 | PhCH2CH2(CO)His-Trp-Ala-Val-DAla-His-Sta-Phe-NH2
Type:
Small organic molecule
Emp. Form.:
C60H78N14O10
Mol. Mass.:
1155.3491
SMILES:
CC(C)CC(NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1ccccc1)C(C)C)C(O)CC(=O)N[C@@H](Cc1ccccc1)C(N)=O
Structure:
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