grepafloxacin [Ligand Id: 10818] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL583 (Raxar, Grepafloxacin)
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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 Inhibition of human ERG in MCF7 cells B 4.11 pIC50 77624.71 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 4.11 pIC50 77624.71 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG B 4.3 pIC50 50118.72 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibitory concentration against potassium channel HERG B 4.3 pIC50 50118.72 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 4.3 pIC50 50118.72 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 4.3 pIC50 50118.72 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG current by patch clamp assay B 4.3 pIC50 50000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3848-3851 [PMID:23711922]
ChEMBL Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay B 4.3 pIC50 >50000 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 5507-5512 [PMID:16931010]
ChEMBL Inhibitory activity against Potassium channel HERG B 4.3 pIC50 50000 nM IC50 J. Med. Chem. (2003) 46: 2017-2022 [PMID:12747773]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against blood stage form of Plasmodium falciparum assessed as incorporation of [3H]hypoxanthine after 72 hrs by liquid scintillation counting F 4.7 pIC50 20000 nM IC50 Eur. J. Med. Chem. (2014) 77: 280-287 [PMID:24650715]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 F 5 pIC50 >=10000 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 F 5 pIC50 >=10000 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against liver stages of Plasmodium falciparum NF54 in mouse after 72 to 120 hrs by immunofluorescence assay F 5 pIC50 10000 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]
Plasmodium yoelii yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612328]
ChEMBL Antimalarial activity against liver stages of Plasmodium yoelii yoelii 265 BY infected in mouse after 48 hrs by immunofluorescence assay F 5 pIC50 10000 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]

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]