tramadol [Ligand Id: 8286] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1237044 (Amanda, CG-315E, E-265, ETS-6103, ETS6103, Tramadol, U-26255A, Ultracet, Ultram)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
There should be some charts here, you may need to enable JavaScript!
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]Naltrindole form human delta opioid receptor expressed in CHO cells B 8.03 pKi 9.4 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb Displacement of the delta antagonist naltrindole from the delta receptor expressed in CHO cells. - 8.03 pKi 9.4 nM Ki Bioorg Med Chem Lett (2009) 19: 203-8 [PMID:19027293]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb Displacement of the kappa agonist U69593 from the kappa receptor expressed in CHO cells. - 7.85 pKi 14 nM Ki Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]
ChEMBL Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells B 7.85 pKi 14 nM Ki 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 Opioid receptor mu 1 agonist activity with monoamine (NE, 5-HT) uptake-blocking activity in the 0.8-1 uM range F 5.7 pKi 2000 nM Ki J Med Chem (1999) 42: 1481-1500 [PMID:10229619]
ChEMBL Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells B 5.8 pKi 1600 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb Displacement of the mu aginist peptide DAMGO from the mu receptor expressed in CHO cells. - 5.8 pKi 1600 nM Ki Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]
ChEMBL Inhibition of mu opioid receptor B 5.12 pIC50 7600 nM IC50 Bioorg Med Chem Lett (2006) 16: 691-694 [PMID:16257206]
ChEMBL Binding affinity to mu opioid receptor B 5.12 pIC50 7600 nM IC50 Bioorg Med Chem Lett (2008) 18: 1674-1680 [PMID:18242987]
ChEMBL Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay F 5.89 pEC50 1300 nM EC50 ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459]
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 5.62 pKi 2400 nM Ki Eur J Med Chem (2011) 46: 4992-4999 [PMID:21864951]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibition of NET mediated norepinephrine uptake B 5.41 pIC50 3861 nM IC50 Bioorg Med Chem Lett (2008) 18: 1674-1680 [PMID:18242987]
ChEMBL Inhibition of reuptake of Norepinephrine B 6.1 pIC50 790 nM IC50 Bioorg Med Chem Lett (2006) 16: 691-694 [PMID:16257206]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.7 pKi 198 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of reuptake of 5HT B 5.37 pIC50 4300 nM IC50 Bioorg Med Chem Lett (2006) 16: 691-694 [PMID:16257206]
ChEMBL Inhibition of SERT mediated 5-hydroxytryptamine uptake B 5.83 pIC50 1493 nM IC50 Bioorg Med Chem Lett (2008) 18: 1674-1680 [PMID:18242987]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.43 pIC50 372 nM IC50 DrugMatrix in vitro pharmacology data
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 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.28 pIC50 52500 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]

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]