butorphanol [Ligand Id: 7591] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL33986 (Butorphanol, LEVO-BC-2627)
  • 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 Displacement of [3H]Naltindole from human delta opioid receptor expressed in CHO cell membrane B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2008) 18: 4474-4476 [PMID:18674902]
ChEMBL Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL Displacement of [3H]naltrindole from human delta-opioid receptor expressed in CHO cells after 3 hrs by scintillation counting B 7.92 pKi 12 nM Ki Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells B 9.66 pKi 0.22 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb Displacement of [3H]U69593 from human κ opioid receptor expressed in CHO cells. - 9.92 pKi 0.12 nM Ki Bioorg Med Chem Lett (2008) 18: 4474-6 [PMID:18674902]
ChEMBL Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cell membrane B 9.92 pKi 0.12 nM Ki Bioorg Med Chem Lett (2008) 18: 4474-4476 [PMID:18674902]
ChEMBL Displacement of [3H]U69563 from human kappa-opioid receptor expressed in CHO cells after 60 mins by scintillation counting B 9.92 pKi 0.12 nM Ki Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
ChEMBL Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 8.54 pEC50 2.9 nM EC50 Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
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 CHO cell membrane B 9.66 pKi 0.22 nM Ki Bioorg Med Chem Lett (2008) 18: 4474-4476 [PMID:18674902]
ChEMBL Displacement of [3H]DAMGO from human mu-opioid receptor expressed in CHO cells after 60 mins by scintillation counting B 9.66 pKi 0.22 nM Ki Bioorg Med Chem (2011) 19: 2808-2816 [PMID:21482470]
GtoPdb Displacement of [3H]DAMGO from human μ opioid receptor expressed in CHO cells. - 9.92 pKi 0.12 nM Ki Bioorg Med Chem Lett (2008) 18: 4474-6 [PMID:18674902]
ChEMBL Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells B 9.92 pKi 0.12 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL Activity at human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding F 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]