tapentadol [Ligand Id: 7477] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1201776 (BN-200, BN 200 (BASE), CG-5503, CG5503, CG5503 (BASE), CG5503 IR, NSC-759619, Tapentadol)
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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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  • NET in Human [GtoPdb: 926] [UniProtKB: P23975]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK-293 cells by scintillation counting B 6.8 pKi 160 nM Ki ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459]
GtoPdb - - 6.8 pKi 160 nM Ki J Pharmacol Exp Ther (2007) 323: 265-76 [PMID:17656655]
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 6.17 pEC50 670 nM EC50 ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459]
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 4.66 pIC50 21890 nM IC50 J Med Chem (2019) 62: 9890-9905 [PMID:31597043]
NET in Human [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 5.06 pKi 8800 nM Ki J Pharmacol Exp Ther (2007) 323: 265-76 [PMID:17656655]

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]