levomilnacipran [Ligand Id: 7435] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL99946 ((1s,2r)-milnacipran, F 2695, F-2695, F2695, Fetzima, Levomilnacipran, Milnacipran, (1s,2r)-) |
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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] | ||||||||
| GtoPdb | - | - | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3230-5 [PMID:18468895] |
| ChEMBL | Inhibition of human DAT | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3328-3332 [PMID:18445525] |
| ChEMBL | Inhibition of dopamine uptake at human DAT expressed in HEK293 cells | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3230-3235 [PMID:18468895] |
| GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| ChEMBL | Binding affinity for N-methyl-D-aspartate glutamate receptor of cerebral cortical synaptic membranes from rats using [3H]MK-801 as radioligand | B | 5.2 | pIC50 | 6300 | nM | IC50 | J Med Chem (2003) 46: 5326-5333 [PMID:14640541] |
| ChEMBL | Inhibition of [3H]-MK-801 binding to NMDA receptor from rat cerebral cortical synaptic membrane | B | 5.2 | pIC50 | 6300 | nM | IC50 | J Med Chem (1996) 39: 4844-4852 [PMID:8941398] |
| ChEMBL | Inhibition of [3H]MK-801 binding to N-methyl-D-aspartate glutamate receptor of rat cerebral cortical synaptic membrane | B | 5.2 | pIC50 | 6300 | nM | IC50 | J Med Chem (1998) 41: 3507-3514 [PMID:9719604] |
| ChEMBL | Inhibition of [3H]MK-801 binding to NMDA receptor of rat cerebral cortical synaptic membrane | B | 5.2 | pIC50 | 6300 | nM | IC50 | J Med Chem (1995) 38: 2964-2968 [PMID:7636857] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Inhibition of human NET | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3328-3332 [PMID:18445525] |
| ChEMBL | Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3230-3235 [PMID:18468895] |
| GtoPdb | - | - | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3230-5 [PMID:18468895] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| GtoPdb | - | - | 6.49 | pIC50 | 320 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3230-5 [PMID:18468895] |
| ChEMBL | Inhibition of human SERT | B | 6.49 | pIC50 | 320 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3328-3332 [PMID:18445525] |
| ChEMBL | Inhibition of serotonin uptake at human SERT expressed in HEK293 cells | B | 6.49 | pIC50 | 320 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3230-3235 [PMID:18468895] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Inhibition of [3H]-paroxetine binding on serotonin transporter of rat cerebral cortical synaptic membrane | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1996) 39: 4844-4852 [PMID:8941398] |
| ChEMBL | Inhibition of Serotonin transporter in cerebral cortical synaptic membrane of rats using [3H]paroxetine | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1998) 41: 3507-3514 [PMID:9719604] |
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]
