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TargetMu-type opioid receptor
LigandBDBM21019
Substrate/CompetitorBDBM21015
Meas. Tech.Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 27±n/a nM
EC50 42±n/a nM
Citation Yamamoto, TNair, PDavis, PMa, SWNavratilova, EMoye, STumati, SLai, JVanderah, TWYamamura, HIPorreca, FHruby, VJ Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. J Med Chem50:2779-86 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Mu-type opioid receptor
Name:Mu-type opioid receptor
Synonyms:MOR-1 | MUOR1 | Mu-type opioid receptor (MOR) | OPIATE Mu | OPRM_RAT | Opiate non-selective | Opioid receptor B | Oprm1 | Ror-b
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:44503.11
Organism:Rattus norvegicus (rat)
Description:Competition binding assays were carried out using membrane preparations from transfected HN9.10 cells that constitutively expressed the mu opioid receptor.
Residue:398
Sequence:
MDSSTGPGNTSDCSDPLAQASCSPAPGSWLNLSHVDGNQSDPCGLNRTGLGGNDSLCPQT
GSPSMVTAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATST
LPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRT
PRNAKIVNVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFA
FIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYV
IIKALITIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSTIEQ
QNSTRVRQNTREHPSTANTVDRTNHQLENLEAETAPLP
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BDBM21019
BDBM21015
NameBDBM21019
Synonyms:Bifunctional Peptide Ligand, 3 (TY006) | H-Tyr-D-Ala-Gly-Phe-Gly-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | [3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-[(2S)-2-{[(2S)-1-{2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanamido]acetyl}pyrrolidin-2-yl]formamido}-4-methylpentanamido]-3-(1H-indol-3-yl)propanoate
TypePeptide-like ligand
Emp. Form.C56H63F6N9O10
Mol. Mass.1136.1441
SMILESCC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(cc(c1)C(F)(F)F)C(F)(F)F
Structure
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