milnacipran [Ligand Id: 7436] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL259209 (Impulsor, Midalcipran, Milnacipran) |
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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 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]
