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ChEMBL ligand: CHEMBL583 (Grepafloxacin, Raxar) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]