tramadol [Ligand Id: 8286] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1237044 (Amanda, CG-315E, E-265, ETS-6103, ETS6103, Tramadol, U-26255A, Ultracet, Ultram) |
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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]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 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]
