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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 |
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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]