milnacipran [Ligand Id: 7436] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL259209 (Impulsor, Midalcipran, Milnacipran)
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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]
ChEMBL Displacement of [3H]WIN35428 from human recombinant DAT transfected in HEK293 cell membrane B 4.5 pKi >31622.78 nM Ki Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683]
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]
ChEMBL Inhibition of dopamine uptake at human DAT expressed in HEK293 cells B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2008) 18: 3230-3235 [PMID:18468895]
ChEMBL Inhibition of human DAT B 5.21 pIC50 6100 nM IC50 Bioorg Med Chem Lett (2008) 18: 1346-1349 [PMID:18207394]
ChEMBL Inhibition of human DAT B 5.21 pIC50 6100 nM IC50 Bioorg Med Chem Lett (2008) 18: 3328-3332 [PMID:18445525]
ChEMBL Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter B 5.21 pIC50 6100 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from rat synaptosomal DAT expressed in HEK293 cells by microplate scintillation counter B 4.43 pIC50 37000 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]
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 7.07 pKi 85 nM Ki ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells B 5.26 pIC50 5500 nM IC50 Bioorg Med Chem Lett (2008) 18: 3230-3235 [PMID:18468895]
ChEMBL Inhibition of human NET B 7.11 pIC50 77 nM IC50 Bioorg Med Chem Lett (2008) 18: 1346-1349 [PMID:18207394]
ChEMBL Inhibition of human NET B 7.11 pIC50 77 nM IC50 Bioorg Med Chem Lett (2008) 18: 3328-3332 [PMID:18445525]
ChEMBL Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter B 7.11 pIC50 77 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]
ChEMBL Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 7.39 pIC50 41 nM IC50 ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
GtoPdb - - 9.1 pIC50 0.79 nM IC50 Bioorg Med Chem Lett (2013) 23: 1456-61 [PMID:23347683]
ChEMBL Inhibition of human recombinant NET expressed in HEK293 cells assessed as inhibition of [3H]NE reuptake B 9.1 pIC50 0.79 nM IC50 Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 8.19 pKi 6.5 nM Ki ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL Inhibition of serotonin uptake at human SERT expressed in HEK293 cells B 5.46 pIC50 3500 nM IC50 Bioorg Med Chem Lett (2008) 18: 3230-3235 [PMID:18468895]
ChEMBL Inhibition of human SERT B 6.38 pIC50 420 nM IC50 Bioorg Med Chem Lett (2008) 18: 1346-1349 [PMID:18207394]
ChEMBL Inhibition of human SERT B 6.38 pIC50 420 nM IC50 Bioorg Med Chem Lett (2008) 18: 3328-3332 [PMID:18445525]
ChEMBL Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter B 6.38 pIC50 420 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]
ChEMBL Inhibitory concentration against serotonin transporter B 7 pIC50 100 nM IC50 J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL Inhibition of human recombinant SERT expressed in HEK293 cells assessed as inhibition of [3H]5HT reuptake B 7.3 pIC50 50.12 nM IC50 Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683]
GtoPdb - - 7.3 pIC50 50.12 nM IC50 Bioorg Med Chem Lett (2013) 23: 1456-61 [PMID:23347683]
ChEMBL Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis B 7.66 pIC50 22 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 7.57 pKi 27 nM Ki ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL Inhibition of radiolabeled serotonin uptake from rat brain SERT B 6.69 pIC50 203 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]
ChEMBL Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from rat synaptosomal SERT expressed in HEK293 cells by microplate scintillation counter B 7.33 pIC50 47 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL Inhibition of radiolabeled noradrenaline uptake from rat brain NET B 7 pIC50 100 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]
ChEMBL Displacement of Levo[ring-2,5,6-3H]norepinephrine from rat synaptosomal NET expressed in HEK293 cells by microplate scintillation counter B 7.52 pIC50 30 nM IC50 J Med Chem (2008) 51: 7265-7272 [PMID:18954038]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]