etonitazene [Ligand Id: 1624] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL312040 (Acscn-9624, Arc 1g2, BA-20684, Ciba 20-684ba, Etobedolum, Etonitazene, Etonitazine, IDS-NE-006, NIH 7607, NIH-7607)
  • δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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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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  • Mu-type opioid receptor in Rhesus macaque [ChEMBL: CHEMBL5799] [UniProtKB: Q9MYW9]
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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 in Human [GtoPdb: 317] [UniProtKB: P41143]
GtoPdb - - 6.7 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Opioid receptor delta 1 apparent binding constant from rat brain membranes using [3H]DADLE binding assay B 6 pKi >1000 nM Ki J Med Chem (1990) 33: 2456-2464 [PMID:2167979]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]-Diprenorphine from human mu opioid receptor expressed in HEK293-TSA cell membranes after 4 hrs by scintillation counting method B 9.7 pKi 0.2 nM Ki J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
GtoPdb - - 9.7 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
GtoPdb Potency determined as inhibition of cAMP accumulation in a Gi-cAMP assay - 10.52 pEC50 0.03 nM EC50 Psychopharmacology (Berl) (2023) 240: 2573-2584 [PMID:37658878]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
GtoPdb Binding affinity determined in radioligand displacement assay using rat brain and [3H]DAMGO as tracer - 8.18 pKi 6.6 nM Ki Psychopharmacology (Berl) (2023) 240: 2573-2584 [PMID:37658878]
ChEMBL Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1 B 9.3 pKi 0.5 nM Ki J Med Chem (1990) 33: 2456-2464 [PMID:2167979]
Mu-type opioid receptor in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5799] [UniProtKB: Q9MYW9]
ChEMBL Binding affinity to mu opioid receptor in rhesus monkey brain membrane in absence of Na+ ions B 10.7 pKi 0.02 nM Ki Eur J Med Chem (2008) 43: 2307-2315 [PMID:18403056]
ChEMBL Binding affinity to mu opioid receptor in rhesus monkey brain membrane in presence of Na+ ions B 11 pKi 0.01 nM Ki Eur J Med Chem (2008) 43: 2307-2315 [PMID:18403056]
κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb - - 6.9 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]

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]