methadone [Ligand Id: 5458] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL651 (Methadose, Phy, Westadone, Methadone, Amidone, Symoron, Heptadon, Dolophine, IDS-NM-002, Physeptone)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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]
ChEMBL Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand B 5.96 pIC50 1090 nM IC50 J. Med. Chem. (2001) 44: 3378-3390 [PMID:11585443]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibitory concentration against potassium channel HERG B 5.01 pIC50 9772.37 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand B 6.29 pIC50 512 nM IC50 J. Med. Chem. (2001) 44: 3378-3390 [PMID:11585443]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand B 8.39 pIC50 4.1 nM IC50 J. Med. Chem. (2001) 44: 3378-3390 [PMID:11585443]
GtoPdb Binding affinity against μ-opioid receptor (human) using [3H]DAMGO radioligand. - 8.39 pIC50 4.1 nM IC50 J Med Chem (2001) 44: 3378-90 [PMID:11585443]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 transepithelial transport (basal to apical) (Rhodamine 123: 5 uM) in Caco-2 cells F 5.12 pIC50 7500 nM IC50 Drug Metab. Dispos. (2001) 29: 954-956 [PMID:11408360]

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]