moxifloxacin [Ligand Id: 10915] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL32 (Avelox, Avelox i.v., Avelox iv, Moxifloxacin, Vigamox, Zimoxin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DNA gyrase subunit A/DNA gyrase subunit B/DNA gyrase in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094139] [GtoPdb: 3217, 3218] [UniProtKB: P0AES4, P0AES6] | ||||||||
| ChEMBL | Inhibition of Escherichia coli DNA gyrase GyrA/GyrB | B | 5.6 | pIC50 | 2500 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 2909-2914 [PMID:18426901] |
| ChEMBL | Inhibitory activity against wild type Escherichia coli gyrase | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 1272-1276 [PMID:16337791] |
| DNA gyrase in S.aureus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038482] [UniProtKB: P0A0K8, P20831] | ||||||||
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase by supercoiling assay | B | 4.55 | pIC50 | 28000 | nM | IC50 | J Med Chem (2007) 50: 199-210 [PMID:17228862] |
| ChEMBL | Inhibition of Staphylococcus aureus wild-type DNA gyrase supercoiling activity assessed as effect on conversion of relaxed pBR322 DNA to supercoiled form | B | 4.56 | pIC50 | 27500 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2445-2453 [PMID:17502409] |
| ChEMBL | Inhibition of Staphylococcus aureus DNA gyrase by supercoiling assay | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2011) 54: 3418-3425 [PMID:21443219] |
| ChEMBL | Inhibition of wild-type Staphylococcus aureus DNA gyrase assessed as inhibition of supercoiling of pBR322 DNA after 60 min by gel electrophoresis assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | J Med Chem (2011) 54: 3268-3282 [PMID:21425851] |
| DNA gyrase subunit A in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4165] [UniProtKB: P9WG47] | ||||||||
| ChEMBL | Inhibition of DNA supercoiling activity of Mycobacterium tuberculosis DNA gyrase subunit A D94G mutant | B | 4.23 | pIC50 | 59000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3478-3480 [PMID:20516287] |
| ChEMBL | Inhibition of DNA supercoiling activitysof Mycobacterium tuberculosis DNA gyrase subunit A A90V mutant | B | 4.51 | pIC50 | 31000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3478-3480 [PMID:20516287] |
| ChEMBL | Inhibition of DNA supercoiling activity of wild type Mycobacterium tuberculosis DNA gyrase A | B | 5.04 | pIC50 | 9200 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3478-3480 [PMID:20516287] |
| DNA gyrase subunit A/DNA gyrase subunit B in Mycobacterium tuberculosis (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430898] [UniProtKB: P9WG45, P9WG47] | ||||||||
| ChEMBL | Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase assessed as supercoiling of pBR322 DNA after 90 mins by agarose gel electrophoresis method | B | 4.9 | pIC50 | 12500 | nM | IC50 | ACS Med Chem Lett (2015) 6: 741-746 [PMID:26191359] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase holoenzyme-mediated supercoiling of pBR322 DNA after 90 mins by agarose gel electrophoresis | B | 4.9 | pIC50 | 12500 | nM | IC50 | J Med Chem (2014) 57: 4889-4905 [PMID:24809953] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling after 30 mins by electrophoresis | B | 4.95 | pIC50 | 11200 | nM | IC50 | Bioorg Med Chem (2016) 24: 877-885 [PMID:26787274] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining and electrophoresis based DNA supercoiling assay | B | 4.95 | pIC50 | 11200 | nM | IC50 | Bioorg Med Chem (2015) 23: 2062-2078 [PMID:25801151] |
| ChEMBL | Inhibition of DNA gyrase GyrA/GyrB in Mycobacterium tuberculosis incubated for 30 mins assessed as reduction in supercoiling of relaxed relaxed pBR322 DNA by ethidium bromide staining based agarose gel electrophoresis method | B | 4.95 | pIC50 | 11200 | nM | IC50 | Eur J Med Chem (2015) 103: 1-16 [PMID:26318054] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of supercoiling activity using relaxed pBR322 plasmid as substrate after 30 mins | B | 4.95 | pIC50 | 11200 | nM | IC50 | Bioorg Med Chem (2016) 24: 42-52 [PMID:26678175] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase-mediated relaxed pBR322 DNA supercoiling by gel electrophoresis | B | 5 | pIC50 | 10000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1005-1009 [PMID:25221657] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase supercoiling activity using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining method | B | 5.09 | pIC50 | 8100 | nM | IC50 | Bioorg Med Chem (2014) 22: 4924-4934 [PMID:25129171] |
| ChEMBL | Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB | B | 5.22 | pIC50 | 6000 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 2909-2914 [PMID:18426901] |
| DNA gyrase subunit B in Mycobacterium smegmatis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085613] [UniProtKB: P0C559] | ||||||||
| ChEMBL | Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem (2014) 22: 4924-4934 [PMID:25129171] |
| ChEMBL | Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2062-2078 [PMID:25801151] |
| ChEMBL | Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2015) 103: 1-16 [PMID:26318054] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay | F | 4.1 | pIC50 | 79432.82 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of human ERG expressed in mammalian cells by patch clamp method | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2011) 54: 3418-3425 [PMID:21443219] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | In vitro inhibitory activity against chloroquine-resistant Plasmodium falciparum NF54-R in blood | F | 4.35 | pIC50 | 45000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2773-2776 [PMID:15125930] |
| 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 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] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | F | 4.4 | pIC50 | 39810.72 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Topoisomerase IV subunit A in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4088] [UniProtKB: P0C1U9] | ||||||||
| ChEMBL | Inhibitory activity against Staphylococcus aureus ATCC 29213 wild type Topo 4 | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 1277-1281 [PMID:16337789] |
| ChEMBL | Inhibitory activity against wild type Staphylococcus aureus topoisomerase 4 | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 1272-1276 [PMID:16337791] |
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]
