grepafloxacin [Ligand Id: 10818] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL583 (Grepafloxacin, Grepafloxacine, Grepafloxacino, Raxar) |
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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] |
| 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 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]
