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

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ChEMBL ligand: CHEMBL651 (Amidone, Diaminon, Dl-methadone, Dolophin, Dolophine, Heptadon, Heptadone, IDS-NM-002, Metasedin, Methadone, Methadose, Phenadone, Phy, Physeptone, Symoron, Westadone)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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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]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 4 pKi >100000 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 5.68 pKi 2110 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 4.58 pKi 26200 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
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 Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay B 7.89 pKi 13 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]