pethidine [Ligand Id: 7221] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL607 (IDS-NP-001, Isonipecaine, Meperidine, Meperidol, Pethanol, Pethidine, Pethidine dbl, Pethidineter, Renaudin)
  • 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]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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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]
GtoPdb - - 5 pIC50 >10000 nM IC50 J Med Chem (2001) 44: 3378-90 [PMID:11585443]
ChEMBL Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand B 5 pIC50 >10000 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Displacement of [3H]WIN-35428 from dopamine transporter (DAT) B 4.75 pKi 17800 nM Ki Bioorg Med Chem Lett (1999) 9: 3273-3276 [PMID:10612583]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG channel in HEK293 cells by voltage-clamp method B 4.12 pIC50 75857.76 nM IC50 Eur J Med Chem (2008) 43: 2479-2488 [PMID:18262683]
ChEMBL Inhibition of human ERG B 4.13 pIC50 74131.02 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibitory concentration against potassium channel HERG B 6.49 pIC50 323.59 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 5.63 pIC50 2370 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
GtoPdb - - 5.63 pIC50 2370 nM IC50 J Med Chem (2001) 44: 3378-90 [PMID:11585443]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity against Opioid receptor kappa 1 was determined in brain membrane preparations from male Hartley guinea-pigs B 4 pKi >100000 nM Ki Bioorg Med Chem Lett (1998) 8: 1813-1818 [PMID:9873439]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb - - 6.5 pIC50 315 nM IC50 J Med Chem (2001) 44: 3378-90 [PMID:11585443]
ChEMBL Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand B 6.5 pIC50 315 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL Agonist activity at human cloned mu opioid receptor by [35S]GTPgammaS binding assay F 5.03 pEC50 9400 nM EC50 Bioorg Med Chem Lett (2009) 19: 1228-1232 [PMID:19168350]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Binding affinity against mu opioid receptor was determined in brain membrane preparations from male Hartley guinea-pigs B 6.35 pKi 451 nM Ki Bioorg Med Chem Lett (1998) 8: 1813-1818 [PMID:9873439]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Displacement of [3H]paroxetine from serotonin transporter (SERT) B 6.39 pKi 412 nM Ki Bioorg Med Chem Lett (1999) 9: 3273-3276 [PMID:10612583]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis B 4.65 pIC50 22250 nM IC50 J Med Chem (2019) 62: 9890-9905 [PMID:31597043]

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]