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ChEMBL ligand: CHEMBL814 (Fluvoxamine, N06AB08) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]