levomilnacipran [Ligand Id: 7435] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL99946 (Levomilnacipran, Fetzima, F-2695, F2695, F 2695)
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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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]
GtoPdb - - 5.49 pIC50 3200 nM IC50 Bioorg Med Chem Lett (2008) 18: 3230-5 [PMID:18468895]
ChEMBL Inhibition of human DAT B 5.49 pIC50 3200 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3328-3332 [PMID:18445525]
ChEMBL Inhibition of dopamine uptake at human DAT expressed in HEK293 cells B 5.49 pIC50 3200 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3230-3235 [PMID:18468895]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Binding affinity for N-methyl-D-aspartate glutamate receptor of cerebral cortical synaptic membranes from rats using [3H]MK-801 as radioligand B 5.2 pIC50 6300 nM IC50 J. Med. Chem. (2003) 46: 5326-5333 [PMID:14640541]
ChEMBL Inhibition of [3H]-MK-801 binding to NMDA receptor from rat cerebral cortical synaptic membrane B 5.2 pIC50 6300 nM IC50 J. Med. Chem. (1996) 39: 4844-4852 [PMID:8941398]
ChEMBL Inhibition of [3H]MK-801 binding to N-methyl-D-aspartate glutamate receptor of rat cerebral cortical synaptic membrane B 5.2 pIC50 6300 nM IC50 J. Med. Chem. (1998) 41: 3507-3514 [PMID:9719604]
ChEMBL Inhibition of [3H]MK-801 binding to NMDA receptor of rat cerebral cortical synaptic membrane B 5.2 pIC50 6300 nM IC50 J. Med. Chem. (1995) 38: 2964-2968 [PMID:7636857]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibition of human NET B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3328-3332 [PMID:18445525]
ChEMBL Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3230-3235 [PMID:18468895]
GtoPdb - - 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2008) 18: 3230-5 [PMID:18468895]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 6.49 pIC50 320 nM IC50 Bioorg Med Chem Lett (2008) 18: 3230-5 [PMID:18468895]
ChEMBL Inhibition of human SERT B 6.49 pIC50 320 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3328-3332 [PMID:18445525]
ChEMBL Inhibition of serotonin uptake at human SERT expressed in HEK293 cells B 6.49 pIC50 320 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3230-3235 [PMID:18468895]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of [3H]-paroxetine binding on serotonin transporter of rat cerebral cortical synaptic membrane B 8.07 pKi 8.5 nM Ki J. Med. Chem. (1996) 39: 4844-4852 [PMID:8941398]
ChEMBL Inhibition of Serotonin transporter in cerebral cortical synaptic membrane of rats using [3H]paroxetine B 8.07 pKi 8.5 nM Ki J. Med. Chem. (1998) 41: 3507-3514 [PMID:9719604]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]