milnacipran [Ligand Id: 7436] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL259209 (Impulsor, Midalcipran, Milnacipran) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
