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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
