fluvoxamine [Ligand Id: 7189] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL814 (Fluvoxamina, Fluvoxamine, N06AB08) |
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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 | In vitro competitive binding versus [N-methyl-3H]WIN-35428 in murine kidney cells transfected with cDNA for human dopamine transporter (DAT) | B | 8.84 | pKi | 1.46 | nM | Ki | J Med Chem (2003) 46: 925-935 [PMID:12620070] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibition of dopamine uptake in synaptosomal preparation in rat corpus striatum, using [3H]dopamine | F | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (1984) 27: 1508-1515 [PMID:6492080] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of hERG K channel | F | 5.51 | pIC50 | 3100 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine | F | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1984) 27: 1508-1515 [PMID:6492080] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| GtoPdb | - | - | 8.66 | pKd | 2.2 | nM | Kd | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
| ChEMBL | Displacement of [3H]citalopram from human SERT in HEK293 cells by Topcount scintillation analysis | B | 6.34 | pKi | 458 | nM | Ki | Eur J Med Chem (2021) 220: 113533-113533 [PMID:34049262] |
| ChEMBL | Inhibition constant against [3H]citalopram in murine kidney cells transfected with human dopamine transporter | B | 8.51 | pKi | 3.08 | nM | Ki | J Med Chem (2000) 43: 639-648 [PMID:10691690] |
| ChEMBL | Inhibition of SERT (unknown origin) | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| GtoPdb | Inhibition of [3]5-HT uptake into rat astrocyte cultures. | - | 8.19 | pKi | 6.5 | nM | Ki | Neurochem Int (2001) 39: 39-49 [PMID:11311448] |
| ChEMBL | Inhibition of 5-HT uptake in synaptosomal preparation from rat corpus striatum, using [3H]5-HT | F | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (1984) 27: 1508-1515 [PMID:6492080] |
| σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7] | ||||||||
| ChEMBL | Displacement of [3H]DTG from sigma 2 receptor in Sprague-Dawley rat brain membranes in presence of (+)-pentazocine by scintillation counting method | B | 5.07 | pKi | 8439 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| GtoPdb | Binding affinity. | - | 7.44 | pKi | 36 | nM | Ki |
ACS Med Chem Lett (2012) 3: 1054-1058 [PMID:23641311]; J Clin Psychiatry (2008) 69: 1673-4 [PMID:19200426] |
| ChEMBL | Binding affinity to sigma 1 receptor | B | 7.44 | pKi | 36 | nM | Ki | ACS Med Chem Lett (2012) 3: 1054-1058 [PMID:23641311] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Displacement of [3H]-(+)pentazocine from rat brain sigma 1-type opioid receptor | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (2012) 55: 5350-5360 [PMID:22515405] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Sprague-Dawley rat brain membranes by scintillation counting method | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA | F | 4.4 | pIC50 | 39400 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
| ChEMBL | Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes | F | 5.31 | pIC50 | 4900 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 5.31 | pIC50 | 4900 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
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]
