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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 |
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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]