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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL583 (Grepafloxacin, Raxar)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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]
ChEMBL Antimalarial activity against CQ-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth F 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2020) 11: 1450-1456 [PMID:32676153]
ChEMBL Antimalarial activity against CQ-resistant Plasmodium falciparum NF54-R assessed as inhibition of parasite growth F 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2020) 11: 1450-1456 [PMID:32676153]
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 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]