Reaction Details |
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Target | Mu-type opioid receptor |
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Ligand | BDBM50341316 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_742675 (CHEMBL1769553) |
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Ki | 0.740000±n/a nM |
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Citation | Yamamoto, T; Nair, P; Largent-Milnes, TM; Jacobsen, NE; Davis, P; Ma, SW; Yamamura, HI; Vanderah, TW; Porreca, F; Lai, J; Hruby, VJ Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies. J Med Chem54:2029-38 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50341316 |
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n/a |
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Name | BDBM50341316 |
Synonyms: | (S)-N-((S)-1-((S)-3-(1H-indol-3-yl)-1-oxo-1-(3-(trifluoromethyl)benzylamino)propan-2-ylamino)-4-methyl-1-oxopentan-2-yl)-1-((2S,5S,11R,14S)-14-amino-5-benzyl-2-butyl-15-(4-hydroxy-2,6-dimethylphenyl)-11-methyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecane)pyrrolidine-2-carboxamide | CHEMBL1766206 |
Type | Small organic molecule |
Emp. Form. | C61H77F3N10O9 |
Mol. Mass. | 1151.3209 |
SMILES | CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(c1)C(F)(F)F |r| |
Structure |
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