sparfloxacin [Ligand Id: 10860] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL850 (AT-4140, CI-978, Esparfloxacino, NSC-759641, Spara, Sparfloxacin, Sparfloxacine, Zagam)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.41 pKi 38619.4 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.33 pIC50 47138.4 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to human ERG S624A tetrameric mutant expressed in HEK293 cells assessed as inhibition of tail current measured upon repolarization to -40 mV by patch clamp method B 4.33 pIC50 46900 nM IC50 Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 4.46 pIC50 34400 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Binding affinity to human ERG F656A tandem dimeric mutant expressed in HEK293 cells assessed as inhibition of tail current measured upon repolarization to -120 mV by patch clamp method B 4.47 pIC50 33600 nM IC50 Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922]
ChEMBL Inhibition of human ERG in MCF7 cells B 4.58 pIC50 26302.68 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state F 4.58 pIC50 26302.68 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Binding affinity to wild type human ERG expressed in HEK293 cells assessed as inhibition of tail current measured upon repolarization to -40 mV by patch clamp method B 4.66 pIC50 21700 nM IC50 Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 4.74 pIC50 18197.01 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibitory concentration against potassium channel HERG B 4.74 pIC50 18197.01 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 4.74 pIC50 18197.01 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG current by patch clamp assay B 4.74 pIC50 18000 nM IC50 Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922]

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]