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, Etonitazeno, 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]
Created with Highcharts 10.3.3ValuesChart context menuδ receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuMu opioid receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat024681012Highcharts.com
  • Mu-type opioid receptor in Rhesus macaque [ChEMBL: CHEMBL5799] [UniProtKB: Q9MYW9]
Created with Highcharts 10.3.3ValuesChart context menuMu-type opioid receptorpKd Rhesus macaquepKi Rhesus macaquepIC50 Rhesus macaquepEC50 Rhesus macaque024681012Highcharts.com
  • κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
Created with Highcharts 10.3.3ValuesChart context menuκ receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
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 35:

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]