methylnaltrexone [Ligand Id: 7563] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1186579 (Methylnaltrexone, MRZ-2663)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
GtoPdb - - 6.05 pKi 900 nM Ki Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]
ChEMBL Displacement of [3H]DPN from recombinant human delta opioid receptor expressed in CHOK1 cell membranes B 6.3 pKi 501.19 nM Ki Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Displacement of [3H]DPN from guinea pig kappa opioid receptor expressed in CHOK1 cell membranes B 7.7 pKi 19.95 nM Ki Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DPN from recombinant human mu opioid receptor expressed in CHOK1 cell membranes B 8.1 pKi 7.94 nM Ki Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
GtoPdb Displacement of [3H]DAMGO from human μ opioid receptors expressed in CHO cells - 8.7 pKi 2 nM Ki Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]
κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb - - 8.2 pKi 6.3 nM Ki Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]