toludesvenlafaxine [Ligand Id: 12766] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4227736 (LPM-570065 FREE BASE, LPM570065 FREE BASE, Ly03005, LY-03005, LY03005, ODVP2, Toludesvenlafaxina, Toludesvenlafaxine)
  • DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
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  • NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT/Sodium-dependent serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Binding affinity to DAT (unknown origin) B 6.31 pIC50 491 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL Inhibition of human DAT expressed in CHO cells assessed as reduction of [3H]-DA re-uptake preincubated for 10 mins followed by [3H]-DA addition measured after 10 mins by liquid scintillation counting B 6.31 pIC50 491 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
GtoPdb - - 6.31 pIC50 491 nM IC50 J Med Chem (2019) 62: 10003 [PMID:31617718]
NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Binding affinity to NET (unknown origin) B 6.12 pIC50 763 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL Inhibition of human NET expressed in CHO cells assessed as reduction of [3H]-NE re-uptake preincubated for 10 mins followed by [3H]-NE addition measured after 10 mins by liquid scintillation counting B 6.12 pIC50 763 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
GtoPdb - - 6.12 pIC50 763 nM IC50 J Med Chem (2019) 62: 10003 [PMID:31617718]
SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 6.14 pIC50 723 nM IC50 J Med Chem (2019) 62: 10003 [PMID:31617718]
ChEMBL Binding affinity to SERT (unknown origin) B 6.14 pIC50 723 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL Inhibition of human SERT expressed in CHO cells assessed as reduction of [3H]-5-HT re-uptake preincubated for 10 mins followed by [3H]-5-HT addition measured after 10 mins by liquid scintillation counting B 6.14 pIC50 723 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]

ChEMBL data shown on this page come from version 36:

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]