Reaction Details |
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Target | Mu-type opioid receptor |
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Ligand | BDBM21122 |
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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 | 5.7±n/a nM |
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EC50 | 24±n/a nM |
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Citation | Lee, YS; Petrov, R; Park, CK; Ma, SW; Davis, P; Lai, J; Porreca, F; Vardanyan, R; Hruby, VJ Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors. J Med Chem50:5528-32 (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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BDBM21122 |
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BDBM21015 |
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Name | BDBM21122 |
Synonyms: | (2S)-2-amino-3-(4-hydroxyphenyl)-N-[(1R)-1-[({[(2S)-1-oxo-1-{4-oxo-4-[4-(N-phenylpropanamido)piperidin-1-yl]butanehydrazido}-3-phenylpropan-2-yl]carbamoyl}methyl)carbamoyl]ethyl]propanamide | 4-anilidopiperidine, 17 |
Type | Peptide-like ligand |
Emp. Form. | C41H52N8O8 |
Mol. Mass. | 784.9004 |
SMILES | CCC(=O)N(C1CCN(CC1)C(=O)CCC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1 |
Structure |
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