A topoisomerase inhibitor that inhibits DNA topoisomerase IV, which catalyses ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands.
ChEBI ID: 53559
| Member | Definition | Class |
|---|---|---|
| ciprofloxacin | A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively. | ciprofloxacin zwitterion; ciprofloxacin |
| ciprofloxacin hydrochloride anhydrous | The anhydrous form of the monohydrochloride salt of ciprofloxacin. | ciprofloxacin hydrochloride (anhydrous) |
| coumermycin | A hydroxycoumarin antibiotic that is obtained from Streptomyces rishiriensis and exhibits potent antibacterial and anticancer activity. | coumermycin A1 |
| fleroxacin | A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria. | fleroxacin |
| gemifloxacin | A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position. | gemifloxacin |
| gemifloxacin mesylate | The mesylate salt of gemifloxacin. | gemifloxacin mesylate |
| levofloxacin | An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase. | levofloxacin |
| tosufloxacin, 4-toluene sulfonate | A racemate comprising equimolar amounts of (R)- and (S)-tosufloxacin tosylate. | tosufloxacin tosylate |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 1,474 (7.68) | 18.7374 |
| 1990's | 3,585 (18.68) | 18.2507 |
| 2000's | 5,367 (27.96) | 29.6817 |
| 2010's | 6,326 (32.96) | 24.3611 |
| 2020's | 2,442 (12.72) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,025 (9.44%) | 5.53% |
| Reviews | 984 (4.59%) | 6.00% |
| Case Studies | 2,687 (12.53%) | 4.05% |
| Observational | 90 (0.42%) | 0.25% |
| Other | 15,655 (73.01%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 27.0842 | 2 | 2 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 26.0678 | 7 | 7 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 18.6954 | 1 | 5 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 28.3708 | 1 | 2 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 30.7369 | 1 | 3 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 69.6219 | 1 | 2 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 30.7369 | 1 | 3 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 100.0000 | 1 | 1 |
| core-binding factor subunit beta isoform 2 | Homo sapiens (human) | Potency | 24.8124 | 3 | 3 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 18.8336 | 1 | 1 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 56.2341 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 15.8822 | 5 | 6 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 24.0133 | 3 | 3 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 27.4376 | 6 | 11 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 12.0840 | 3 | 4 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| GALC protein | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 8.3089 | 2 | 3 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 2.6832 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 12.5893 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| IDH1 | Homo sapiens (human) | Potency | 20.5962 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 3.1272 | 1 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 23.5060 | 2 | 5 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 18.3564 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 3.7578 | 1 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 23.4453 | 2 | 2 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 26.6011 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 12.7755 | 1 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 9.5018 | 2 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 23.9145 | 1 | 1 |
| runt-related transcription factor 1 isoform AML1b | Homo sapiens (human) | Potency | 24.8124 | 3 | 3 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 26.6795 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 26.7764 | 1 | 3 |
| TDP1 protein | Homo sapiens (human) | Potency | 11.6246 | 2 | 12 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 56.2341 | 1 | 1 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 22.4209 | 2 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 23.9145 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 4 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 518.5556 | 4 | 9 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 4 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 43.8628 | 2 | 2 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 29.3452 | 3 | 3 |
| DNA gyrase subunit A | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 6.3000 | 1 | 1 |
| DNA gyrase subunit A | Escherichia coli K-12 | IC50 | 5.4047 | 26 | 27 |
| DNA gyrase subunit A | Mycobacterium tuberculosis H37Rv | IC50 | 118.3876 | 6 | 6 |
| DNA gyrase subunit A | Staphylococcus aureus | IC50 | 99.6681 | 20 | 26 |
| DNA gyrase subunit B | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 6.3000 | 1 | 1 |
| DNA gyrase subunit B | Escherichia coli K-12 | IC50 | 0.5604 | 21 | 22 |
| DNA gyrase subunit B | Mycobacterium tuberculosis H37Rv | IC50 | 24.1628 | 2 | 2 |
| DNA gyrase subunit B | Staphylococcus aureus | IC50 | 46.9668 | 15 | 19 |
| DNA primase | Mycobacterium tuberculosis CDC1551 | IC50 | 75.0000 | 1 | 1 |
| DNA topoisomerase 2-alpha | Homo sapiens (human) | IC50 | 169.8667 | 3 | 3 |
| DNA topoisomerase 4 subunit A | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 1.7000 | 1 | 1 |
| DNA topoisomerase 4 subunit A | Escherichia coli K-12 | IC50 | 51.0000 | 1 | 1 |
| DNA topoisomerase 4 subunit A | Staphylococcus aureus | IC50 | 5.1373 | 10 | 11 |
| DNA topoisomerase 4 subunit B | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 1.7000 | 1 | 1 |
| DNA topoisomerase 4 subunit B | Staphylococcus aureus | IC50 | 6.4850 | 6 | 6 |
| Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | IC50 | 1,600.0000 | 2 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | IC50 | 50.2050 | 2 | 4 |
| Integrase | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| Multidrug and toxin extrusion protein 1 | Homo sapiens (human) | IC50 | 17.9000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 118.0500 | 1 | 4 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 1,551.0003 | 13 | 17 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 125.0000 | 1 | 2 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | IC50 | 7.6000 | 1 | 1 |
| Tubulin alpha-1A chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin alpha-1B chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin alpha-1C chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin alpha-3C chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin alpha-3E chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin alpha-4A chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-1 chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-2A chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-2B chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-3 chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-4A chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-4B chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-6 chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Tubulin beta-8 chain | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Multidrug resistance protein MdtK | Escherichia coli K-12 | Kd | 90.9000 | 1 | 1 |
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 | 0.9210 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Km | 4,300.0000 | 2 | 2 |
| CAAX prenyl protease 2 isoform 2 | Homo sapiens (human) | AC50 | 41.0000 | 1 | 1 |
| DNA gyrase subunit A | Escherichia coli K-12 | Activity | 10.7200 | 4 | 4 |
| DNA gyrase subunit A | Staphylococcus aureus | CC50 | 101.6667 | 3 | 3 |
| DNA gyrase subunit A | Escherichia coli K-12 | EC | 1.2000 | 1 | 1 |
| DNA gyrase subunit B | Escherichia coli K-12 | Activity | 0.4000 | 1 | 1 |
| DNA gyrase subunit B | Staphylococcus aureus | CC50 | 5.0000 | 1 | 1 |
| DNA gyrase subunit B | Escherichia coli K-12 | EC | 1.2000 | 1 | 1 |
| DNA topoisomerase 2-alpha | Homo sapiens (human) | Activity | 104.0000 | 1 | 1 |
| DNA topoisomerase 2-alpha | Homo sapiens (human) | CC50 | 150.0000 | 1 | 1 |
| DNA topoisomerase 2-alpha | Homo sapiens (human) | EC2 | 150.0000 | 1 | 2 |
| DNA topoisomerase 4 subunit A | Staphylococcus aureus | CC50 | 0.4000 | 1 | 1 |
| DNA topoisomerase 4 subunit B | Staphylococcus aureus | CC50 | 0.4000 | 1 | 1 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Mycobacterium tuberculosis H37Rv | MIC | 5.4850 | 2 | 2 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | INH | 18.0000 | 1 | 1 |