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) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DAT/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/Norepinephrine 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/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 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]
