Reaction Details |
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Target | Mu-type opioid receptor |
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Ligand | BDBM50102710 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_149628 (CHEMBL873926) |
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Ki | 171±n/a nM |
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Citation | Thomas, JB; Atkinson, RN; Rothman, RB; Fix, SE; Mascarella, SW; Vinson, NA; Xu, H; Dersch, CM; Lu, Y; Cantrell, BE; Zimmerman, DM; Carroll, FI Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. J Med Chem44:2687-90 (2001) [PubMed] |
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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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BDBM50102710 |
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n/a |
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Name | BDBM50102710 |
Synonyms: | 3-(4-Hydroxy-phenyl)-N-{(S)-1-[(3R,4R)-4-(3-hydroxy-phenyl)-3,4-dimethyl-piperidin-1-ylmethyl]-2-methyl-propyl}-propionamide | 3-(4-Hydroxy-phenyl)-N-{1-[4-(3-hydroxy-phenyl)-3,4-dimethyl-piperidin-1-ylmethyl]-2-methyl-propyl}-propionamide | CHEMBL10986 |
Type | Small organic molecule |
Emp. Form. | C27H38N2O3 |
Mol. Mass. | 438.6022 |
SMILES | CC(C)[C@@H](CN1CC[C@](C)([C@@H](C)C1)c1cccc(O)c1)NC(=O)CCc1ccc(O)cc1 |
Structure |
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