desvenlafaxine [Ligand Id: 7158] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1118 (Desvenlafaxine, D-veniz, Khedezla, Mdd-xr, Newven, O-desmethylvenlafaxine, ODV, Pristiq)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain B 7.22 pIC50 60 nM IC50 J. Med. Chem. (1990) 33: 2899-2905 [PMID:1976813]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Displacement of [3H]WIN35428 from human DAT transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 6.07 pKi >854 nM Ki ACS Med. Chem. Lett. (2013) 4: 560-564 [PMID:24900709]
GtoPdb - - 6.07 pKi >854 nM Ki ACS Med Chem Lett (2013) 4: 560-4 [PMID:24900709]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 6.19 pKi >650 nM Ki ACS Med. Chem. Lett. (2013) 4: 560-564 [PMID:24900709]
GtoPdb - - 6.19 pKi >650 nM Ki ACS Med Chem Lett (2013) 4: 560-4 [PMID:24900709]
ChEMBL Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 5.82 pIC50 1500 nM IC50 ACS Med. Chem. Lett. (2013) 4: 560-564 [PMID:24900709]
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 6.27 pIC50 538 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes F 5.94 pIC50 1160 nM IC50 J. Med. Chem. (1990) 33: 2899-2905 [PMID:1976813]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 7.82 pKi 15 nM Ki ACS Med Chem Lett (2013) 4: 560-4 [PMID:24900709]
ChEMBL Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 7.82 pKi 15 nM Ki ACS Med. Chem. Lett. (2013) 4: 560-564 [PMID:24900709]
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 7.28 pIC50 53 nM IC50 J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 7.77 pIC50 17 nM IC50 ACS Med. Chem. Lett. (2013) 4: 560-564 [PMID:24900709]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Displacement of [3H]-citalopram from Sprague-Dawley rat brain SERT after 1 hr B 6.49 pKi >324 nM Ki ACS Med. Chem. Lett. (2013) 4: 560-564 [PMID:24900709]
ChEMBL Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes F 6.74 pIC50 180 nM IC50 J. Med. Chem. (1990) 33: 2899-2905 [PMID:1976813]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]