moxifloxacin [Ligand Id: 10915] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL32 (Avelox, Avelox i.v., Avelox iv, Moxifloxacin, Moxifloxacine, Moxifloxacino, 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] |
| ChEMBL | Inhibition of Staphylococcus aureus ATTC 25923 DNA gyrase | B | 5.17 | pIC50 | 6800 | nM | IC50 | J Med Chem (2022) 65: 6903-6925 [PMID:35500229] |
| 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 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 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 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 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 Mycobacterium tuberculosis H37Rv DNA gyrase | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2022) 65: 6903-6925 [PMID:35500229] |
| 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 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]
