levallorphan [Ligand Id: 7209] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1254682 (Levallorphan, Lorfan, Naloxiphan)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 4.92 pKi 12000 nM Ki Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells B 8.77 pKi 1.69 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells B 8.89 pKi 1.29 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells B 9.32 pKi 0.48 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
GtoPdb Competition binding assay- the calculated Ki varies depending on the radioligand used. - 9.32 pKi 0.48 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4 [PMID:21621410]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Displacement of [3H]-dihydromorphine from mu opioid receptor in rat cerebral cortex by liquid scintillation counting B 9.2 pIC50 0.63 nM IC50 Eur J Med Chem (2011) 46: 4992-4999 [PMID:21864951]

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]