Reaction Details |
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Target | Mu-type opioid receptor |
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Ligand | BDBM21019 |
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Substrate/Competitor | BDBM21015 |
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Meas. Tech. | Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay |
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pH | 7.4±n/a |
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Temperature | 298.15±n/a K |
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Ki | 27±n/a nM |
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EC50 | 42±n/a nM |
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Citation | Yamamoto, T; Nair, P; Davis, P; Ma, SW; Navratilova, E; Moye, S; Tumati, S; Lai, J; Vanderah, TW; Yamamura, HI; Porreca, F; Hruby, 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 |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Mu-type opioid receptor |
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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 |
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BDBM21015 |
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Name | BDBM21019 |
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 |
Type | Peptide-like ligand |
Emp. Form. | C56H63F6N9O10 |
Mol. Mass. | 1136.1441 |
SMILES | CC(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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