nomifensine [Ligand Id: 4792] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL273575 (Linamiphen, Nomifensin, Nomifensine)
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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
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay B 6.96 pKi 109 nM Ki Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Inhibition of DAT B 7.08 pKi 84 nM Ki Bioorg Med Chem Lett (2012) 22: 7219-7222 [PMID:23084899]
ChEMBL Binding affinity to DAT (unknown origin) B 7.1 pKi 79 nM Ki J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL Displacement of [3H]WIN-from cocaine site of dopamine transporter B 7.63 pKi 23.5 nM Ki J Nat Prod (1993) 56: 441-455 [PMID:8496700]
ChEMBL Inhibition of human recombinant DAT expressed in HEK cells B 8 pKi 10 nM Ki ACS Med Chem Lett (2013) 4: 46-51 [PMID:24900562]
ChEMBL Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay B 6.55 pIC50 281.84 nM IC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Inhibition of [3H]dopamine reuptake at human recombinant DAT expressed in COS-7 cells by scintillation counting B 7.5 pIC50 31.62 nM IC50 Bioorg Med Chem Lett (2011) 21: 1434-1437 [PMID:21310612]
ChEMBL Inhibition of dopamine reuptake at DAT expressed in CHO-K1 cells B 7.5 pIC50 31.62 nM IC50 J Med Chem (2011) 54: 5283-5295 [PMID:21739935]
ChEMBL Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting B 7.52 pIC50 30.2 nM IC50 Bioorg Med Chem (2011) 19: 663-676 [PMID:21093273]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Inhibition of dopamine (DA) uptake into rat brain synaptosomes F 7.1 pKi 79 nM Ki J Med Chem (1984) 27: 943-946 [PMID:6747993]
ChEMBL Inhibition of the uptake of tritiated dopamine (DA) in rat synaptosomes B 7.1 pKi 79 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Binding affinity to dopamine transporter (DAT) using [3H]WIN-35428 as a radioligand B 7.37 pKi 42.66 nM Ki J Med Chem (2000) 43: 4151-4159 [PMID:11063611]
ChEMBL Inhibition of DAT in rat synaptosomal membrane B 7.59 pKi 26 nM Ki ACS Med Chem Lett (2013) 4: 46-51 [PMID:24900562]
ChEMBL Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter. B 6.37 pIC50 430 nM IC50 J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL Inhibition of dopamine uptake in synaptosomal preparation in rat corpus striatum, using [3H]dopamine F 6.39 pIC50 410 nM IC50 J Med Chem (1984) 27: 1508-1515 [PMID:6492080]
ChEMBL Inhibition of [3H]dopamine uptake at the dopamine transporter. B 6.62 pIC50 240 nM IC50 J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat striatal synaptosomes by liquid scintillation spectrometry B 6.7 pIC50 200 nM IC50 J Nat Prod (1995) 58: 1475-1484 [PMID:8676127]
ChEMBL Inhibition of [3H]cocaine binding to the dopamine transporter. B 6.92 pIC50 120 nM IC50 J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL Inhibition of [3H]GBR-12935 binding to the dopamine transporter. B 6.94 pIC50 115 nM IC50 J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL Inhibition of [3H]WIN-35428 binding to the dopamine transporter. B 7.34 pIC50 46 nM IC50 J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL Inhibition of [3H]BTCP binding to the dopamine transporter. B 7.47 pIC50 34 nM IC50 J Med Chem (1992) 35: 969-981 [PMID:1552510]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO-K1 cells by electrophysiological assay B 4.57 pIC50 >27000 nM IC50 ACS Med Chem Lett (2013) 4: 46-51 [PMID:24900562]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay B 7.08 pKi 83 nM Ki Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Inhibition of human NET B 7.64 pKi 23 nM Ki Bioorg Med Chem Lett (2012) 22: 7219-7222 [PMID:23084899]
GtoPdb - - 8.1 pKi 7.94 nM Ki
ChEMBL Inhibition of human recombinant NET expressed in HEK cells B 8.3 pKi 5 nM Ki ACS Med Chem Lett (2013) 4: 46-51 [PMID:24900562]
ChEMBL Binding affinity to NET (unknown origin) B 8.42 pKi 3.8 nM Ki J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay B 6.2 pIC50 630.96 nM IC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Inhibition of norepinephrine (NE) into rat brain synaptosomes F 8.42 pKi 3.8 nM Ki J Med Chem (1984) 27: 943-946 [PMID:6747993]
ChEMBL Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes B 8.42 pKi 3.8 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine F 7.7 pIC50 20 nM IC50 J Med Chem (1984) 27: 1508-1515 [PMID:6492080]
ChEMBL Effect on synaptosomal uptake inhibition of Noradrenaline (NA) F 8.18 pIC50 6.6 nM IC50 J Med Chem (1983) 26: 935-947 [PMID:6134833]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Inhibition of SERT B 5.69 pKi 2057 nM Ki Bioorg Med Chem Lett (2012) 22: 7219-7222 [PMID:23084899]
ChEMBL Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay B 5.71 pKi 1930 nM Ki Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL Inhibition of human recombinant SERT expressed in HEK cells B 5.85 pKi 1400 nM Ki ACS Med Chem Lett (2013) 4: 46-51 [PMID:24900562]
ChEMBL Binding affinity to SERT (unknown origin) B 6.06 pKi 874 nM Ki J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay B 5.06 pIC50 8709.64 nM IC50 Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of serotonin (5-HT) uptake into rat brain synaptosomes B 6.06 pKi 874 nM Ki J Med Chem (1984) 27: 943-946 [PMID:6747993]
ChEMBL Inhibition the uptake of tritiated serotonin (5-HT) by the serotonin transporter SERT in rat synaptosomes B 6.06 pKi 874 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Inhibition of 5-HT uptake in synaptosomal preparation from rat corpus striatum, using [3H]5-HT F 5.27 pIC50 5400 nM IC50 J Med Chem (1984) 27: 1508-1515 [PMID:6492080]
ChEMBL Effect on synaptosomal uptake inhibition of 5-hydroxytryptamine (5-HT) F 6.08 pIC50 830 nM IC50 J Med Chem (1983) 26: 935-947 [PMID:6134833]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL Inhibition of rat NET B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2012) 22: 7219-7222 [PMID:23084899]
ChEMBL Inhibition of NET in rat synaptosomal membrane B 8.4 pKi 4 nM Ki ACS Med Chem Lett (2013) 4: 46-51 [PMID:24900562]

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]