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] |
| ChEMBL | Inhibition of DAT (unknown origin) | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2024) 101: 129654-129654 [PMID:38360418] |
| 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] |
| ChEMBL | Inhibition of NET (unknown origin) | B | 7.98 | pIC50 | 10.5 | nM | IC50 | Bioorg Med Chem Lett (2024) 101: 129654-129654 [PMID:38360418] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Inhibition of SERT (unknown origin) | B | 4.72 | pIC50 | 19000 | nM | IC50 | Bioorg Med Chem Lett (2024) 101: 129654-129654 [PMID:38360418] |
| 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 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]
