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) |
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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 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]
