fluvoxamine [Ligand Id: 7189] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL814 (N06AB08, Fluvoxamine)
1 CHEMBL814_lig_chart_1 Dopamine transporter HumanRat
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
2 CHEMBL814_lig_chart_2 HERG Human
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  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
  • This target only has 0 pki data point
  • 0
3 CHEMBL814_lig_chart_3 Norepinephrine transporter Rat
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  • SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
  • SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
  • This target only has 1 pki data point
  • 8.19
4 CHEMBL814_lig_chart_4 SERT HumanRat
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
  • 7.44
5 CHEMBL814_lig_chart_5 Sigma opioid receptor HumanRat
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
  • This target only has 0 pki data point
  • 0
6 CHEMBL814_lig_chart_6 Sodium channel protein type V alpha subunit Human
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
  • This target only has 0 pki data point
  • 0
7 CHEMBL814_lig_chart_7 Voltage-dependent L-type calcium channel subunit alpha-1C Guinea pig
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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 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 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 in Human [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 8.66 pKd 2.2 nM Kd Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
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]
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]
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 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]