nomifensine [Ligand Id: 4792] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL273575 (Linamiphen, Nomifensin, Nomifensine) |
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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 33:
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]
