Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Staphylococcus aureus | DNA gyrase | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Dictyostelium discoideum | DNA topoisomerase II | DNA gyrase | 644 aa | 655 aa | 23.8 % |
Candida albicans | DNA topoisomerase II similar to S. cerevisiae TOP2 (YNL088W) | DNA gyrase | 644 aa | 625 aa | 25.6 % |
Leishmania braziliensis | mitochondrial DNA topoisomerase II | DNA gyrase | 644 aa | 622 aa | 23.8 % |
Mycobacterium leprae | Probable DNA gyrase (subunit B) GyrB (DNA topoisomerase (ATP-hydrolysing)) (DNA topoisomerase II) (Type II DNA topoisomerase) | DNA gyrase | 644 aa | 667 aa | 53.1 % |
Brugia malayi | DNA topoisomerase II, alpha isozyme | DNA gyrase | 644 aa | 659 aa | 24.3 % |
Schistosoma mansoni | DNA topoisomerase II | DNA gyrase | 644 aa | 633 aa | 24.3 % |
Leishmania mexicana | DNA topoisomerase ii | DNA gyrase | 644 aa | 668 aa | 23.1 % |
Trypanosoma cruzi | mitochondrial DNA topoisomerase II, putative | DNA gyrase | 644 aa | 615 aa | 22.6 % |
Trypanosoma cruzi | mitochondrial DNA topoisomerase II, putative | DNA gyrase | 644 aa | 615 aa | 22.6 % |
Leishmania braziliensis | DNA topoisomerase ii | DNA gyrase | 644 aa | 675 aa | 23.0 % |
Plasmodium berghei | DNA gyrase subunit B, putative | DNA gyrase | 644 aa | 662 aa | 36.3 % |
Echinococcus granulosus | DNA topoisomerase 2 alpha | DNA gyrase | 644 aa | 613 aa | 25.9 % |
Leishmania donovani | DNA topoisomerase ii | DNA gyrase | 644 aa | 666 aa | 23.4 % |
Trypanosoma cruzi | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 674 aa | 23.0 % |
Trypanosoma cruzi | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 674 aa | 23.0 % |
Trypanosoma brucei | DNA topoisomerase II alpha, putative | DNA gyrase | 644 aa | 676 aa | 23.4 % |
Onchocerca volvulus | DNA gyrase | 644 aa | 624 aa | 25.8 % | |
Mycobacterium tuberculosis | DNA gyrase (subunit B) GyrB (DNA topoisomerase (ATP-hydrolysing)) (DNA topoisomerase II) (type II DNA topoisomerase) | DNA gyrase | 644 aa | 661 aa | 53.0 % |
Theileria parva | DNA gyrase subunit B, putative | DNA gyrase | 644 aa | 638 aa | 37.1 % |
Onchocerca volvulus | Ectoderm-expressed 4 homolog | DNA gyrase | 644 aa | 673 aa | 24.1 % |
Wolbachia endosymbiont of Brugia malayi | DNA gyrase, topoisomerase II, B subunit, GyrB | DNA gyrase | 644 aa | 561 aa | 50.4 % |
Neospora caninum | hypothetical protein | DNA gyrase | 644 aa | 693 aa | 24.1 % |
Chlamydia trachomatis | DNA gyrase subunit B | DNA gyrase | 644 aa | 561 aa | 55.3 % |
Trypanosoma brucei | DNA topoisomerase II beta, putative | DNA gyrase | 644 aa | 570 aa | 24.0 % |
Mycobacterium ulcerans | DNA gyrase subunit B | DNA gyrase | 644 aa | 663 aa | 54.0 % |
Brugia malayi | Probable DNA topoisomerase II | DNA gyrase | 644 aa | 672 aa | 25.9 % |
Brugia malayi | DNA gyrase/topoisomerase IV, A subunit family protein | DNA gyrase | 644 aa | 548 aa | 25.7 % |
Trypanosoma brucei gambiense | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 619 aa | 25.7 % |
Leishmania infantum | DNA topoisomerase ii | DNA gyrase | 644 aa | 666 aa | 23.6 % |
Babesia bovis | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 587 aa | 22.7 % |
Leishmania major | DNA topoisomerase ii | DNA gyrase | 644 aa | 672 aa | 23.4 % |
Loa Loa (eye worm) | TOPoisomerase family member | DNA gyrase | 644 aa | 668 aa | 26.2 % |
Leishmania major | mitochondrial DNA topoisomerase II | DNA gyrase | 644 aa | 624 aa | 23.1 % |
Onchocerca volvulus | DNA gyrase | 644 aa | 618 aa | 26.5 % | |
Trypanosoma congolense | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 678 aa | 22.7 % |
Plasmodium knowlesi | DNA gyrase subunit B, putative | DNA gyrase | 644 aa | 517 aa | 36.0 % |
Toxoplasma gondii | DNA topoisomerase 2, putative | DNA gyrase | 644 aa | 664 aa | 24.1 % |
Trypanosoma congolense | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 617 aa | 24.8 % |
Entamoeba histolytica | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 544 aa | 25.0 % |
Trypanosoma congolense | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 678 aa | 22.9 % |
Trypanosoma brucei gambiense | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 676 aa | 23.4 % |
Echinococcus multilocularis | DNA topoisomerase 2 alpha | DNA gyrase | 644 aa | 612 aa | 25.8 % |
Candida albicans | DNA topoisomerase II similar to S. cerevisiae TOP2 (YNL088W) | DNA gyrase | 644 aa | 625 aa | 25.6 % |
Plasmodium falciparum | DNA topoisomerase 2 | DNA gyrase | 644 aa | 647 aa | 23.2 % |
Trypanosoma brucei gambiense | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 666 aa | 23.4 % |
Theileria parva | DNA topoisomerase II, putative | DNA gyrase | 644 aa | 683 aa | 23.9 % |
Leishmania donovani | mitochondrial DNA topoisomerase II | DNA gyrase | 644 aa | 624 aa | 23.2 % |
Leishmania mexicana | mitochondrial DNA topoisomerase II | DNA gyrase | 644 aa | 620 aa | 23.4 % |
Leishmania infantum | mitochondrial DNA topoisomerase II | DNA gyrase | 644 aa | 624 aa | 23.2 % |
Trypanosoma brucei | DNA topoisomerase ii | DNA gyrase | 644 aa | 619 aa | 25.7 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Entamoeba histolytica | DNA topoisomerase II, putative | 0.004 | 0.0046 | 0.5 |
Brugia malayi | Copper type II ascorbate-dependent monooxygenase, N-terminal domain containing protein | 0.037 | 0.199 | 0.4822 |
Brugia malayi | DOMON domain containing protein | 0.014 | 0.0634 | 0.15 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0036 | 0.0022 | 0.4736 |
Schistosoma mansoni | dopamine-beta-monooxygenase | 0.1381 | 0.7935 | 1 |
Mycobacterium ulcerans | DNA gyrase subunit B | 0.0072 | 0.0234 | 0.3581 |
Trypanosoma brucei | Lanosterol 14-alpha demethylase | 0.0036 | 0.0022 | 0.4736 |
Loa Loa (eye worm) | DOMON domain-containing protein | 0.014 | 0.0634 | 0.15 |
Schistosoma mansoni | peptidyl-glycine monooxygenase | 0.073 | 0.4102 | 0.5157 |
Trypanosoma brucei | DNA topoisomerase ii | 0.004 | 0.0046 | 1 |
Brugia malayi | Copper type II ascorbate-dependent monooxygenase, C-terminal domain containing protein | 0.073 | 0.4102 | 1 |
Mycobacterium tuberculosis | DNA gyrase (subunit A) GyrA (DNA topoisomerase (ATP-hydrolysing)) (DNA topoisomerase II) (type II DNA topoisomerase) | 0.0136 | 0.0614 | 1 |
Brugia malayi | Copper type II ascorbate-dependent monooxygenase, C-terminal domain containing protein | 0.073 | 0.4102 | 1 |
Echinococcus granulosus | peptidyl glycine alpha amidating monooxygenase | 0.073 | 0.4102 | 1 |
Brugia malayi | DNA gyrase/topoisomerase IV, A subunit family protein | 0.004 | 0.0046 | 0.0059 |
Giardia lamblia | DNA topoisomerase II | 0.0036 | 0.0026 | 0.5 |
Trichomonas vaginalis | DNA topoisomerase II, putative | 0.004 | 0.0046 | 0.5 |
Plasmodium vivax | DNA gyrase subunit A, putative | 0.0136 | 0.0614 | 1 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0036 | 0.0022 | 0.4736 |
Trypanosoma cruzi | mitochondrial DNA topoisomerase II, putative | 0.004 | 0.0046 | 1 |
Plasmodium falciparum | DNA gyrase subunit A | 0.0136 | 0.0614 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.073 | 0.4102 | 1 |
Echinococcus granulosus | DNA topoisomerase 2 alpha | 0.004 | 0.0046 | 0.0059 |
Wolbachia endosymbiont of Brugia malayi | DNA gyrase subunit A | 0.0136 | 0.0614 | 1 |
Brugia malayi | Cytochrome P450 family protein | 0.0057 | 0.0146 | 0.0304 |
Trypanosoma cruzi | Lanosterol 14-alpha demethylase | 0.0036 | 0.0022 | 0.4736 |
Schistosoma mansoni | peptidylglycine monooxygenase | 0.073 | 0.4102 | 0.5157 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0057 | 0.0146 | 0.0304 |
Chlamydia trachomatis | DNA gyrase subunit A | 0.0136 | 0.0614 | 1 |
Loa Loa (eye worm) | DOMON domain-containing protein | 0.014 | 0.0634 | 0.15 |
Brugia malayi | DOMON domain containing protein | 0.014 | 0.0634 | 0.15 |
Leishmania major | cytochrome p450-like protein | 0.0036 | 0.0022 | 0.4736 |
Onchocerca volvulus | 0.014 | 0.0634 | 1 | |
Trypanosoma brucei | cytochrome P450, putative | 0.0036 | 0.0022 | 0.4736 |
Loa Loa (eye worm) | hypothetical protein | 0.073 | 0.4102 | 1 |
Loa Loa (eye worm) | DOMON domain-containing protein | 0.014 | 0.0634 | 0.15 |
Trypanosoma cruzi | cytochrome p450-like protein, putative | 0.0036 | 0.0022 | 0.4736 |
Onchocerca volvulus | 0.014 | 0.0634 | 1 | |
Plasmodium falciparum | DNA gyrase subunit B | 0.0072 | 0.0234 | 0.3308 |
Trypanosoma cruzi | Lanosterol 14-alpha demethylase | 0.0036 | 0.0022 | 0.4736 |
Leishmania major | cytochrome p450-like protein | 0.0036 | 0.0022 | 0.4736 |
Leishmania major | cytochrome p450-like protein | 0.0036 | 0.0022 | 0.4736 |
Brugia malayi | DNA topoisomerase II, alpha isozyme | 0.004 | 0.0046 | 0.0059 |
Treponema pallidum | DNA gyrase, subunit A (gyrA) | 0.0136 | 0.0614 | 1 |
Brugia malayi | DOMON domain containing protein | 0.014 | 0.0634 | 0.15 |
Schistosoma mansoni | DNA topoisomerase II | 0.004 | 0.0046 | 0.0031 |
Brugia malayi | Probable DNA topoisomerase II | 0.004 | 0.0046 | 0.0059 |
Leishmania major | lanosterol 14-alpha-demethylase, putative | 0.0036 | 0.0022 | 0.4736 |
Toxoplasma gondii | DNA gyrase/topoisomerase IV, A subunit domain-containing protein | 0.0136 | 0.0614 | 0.057 |
Brugia malayi | Copper type II ascorbate-dependent monooxygenase, C-terminal domain containing protein | 0.0359 | 0.1925 | 0.4665 |
Mycobacterium leprae | Probable DNA gyrase (subunit A) GyrA (DNA topoisomerase (ATP-hydrolysing)) (DNA topoisomerase II) (Type II DNA topoisomerase) | 0.0065 | 0.0195 | 1 |
Loa Loa (eye worm) | TOPoisomerase family member | 0.004 | 0.0046 | 0.0059 |
Trypanosoma cruzi | mitochondrial DNA topoisomerase II, putative | 0.004 | 0.0046 | 1 |
Echinococcus multilocularis | peptidyl glycine alpha amidating monooxygenase | 0.073 | 0.4102 | 1 |
Plasmodium vivax | DNA gyrase subunit B, putative | 0.0072 | 0.0234 | 0.3308 |
Leishmania major | mitochondrial DNA topoisomerase II | 0.004 | 0.0046 | 1 |
Mycobacterium tuberculosis | DNA gyrase (subunit B) GyrB (DNA topoisomerase (ATP-hydrolysing)) (DNA topoisomerase II) (type II DNA topoisomerase) | 0.0072 | 0.0234 | 0.3581 |
Echinococcus multilocularis | DNA topoisomerase 2 alpha | 0.004 | 0.0046 | 0.0059 |
Mycobacterium ulcerans | DNA gyrase subunit A | 0.0136 | 0.0614 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | Reduction in steady-state levels of supercoiled pUC18 in Escherichia coli CAG12184 tolC mutant | ChEMBL. | 17116675 | |
Activity (functional) | 0 | Reduction in steady-state levels of supercoiled pUC18 in Escherichia coli CAG12184 tolC mutant | ChEMBL. | 17116675 |
Inhibition (functional) | = 20 % | Inhibition of RNA synthesis in Staphylococcus aureus ATCC 29213 assessed as [3H]uridine incorporation | ChEMBL. | 17116675 |
Inhibition (functional) | = 20 % | Inhibition of protein synthesis in Staphylococcus aureus ATCC 29213 assessed as [3H]aminoacid incorporation | ChEMBL. | 17116675 |
Inhibition (functional) | = 80 % | Inhibition of DNA synthesis in Staphylococcus aureus ATCC 29213 assessed as [3H]thymidine incorporation | ChEMBL. | 17116675 |
Ki (binding) | = 0.044 uM | Inhibition of Staphylococcus aureus DNA gyrase | ChEMBL. | 18690678 |
MIC (functional) | = 0.5 ug ml-1 | Antibacterial activity against Streptococcus pneumoniae ATCC BAA-255 after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 0.5 ug ml-1 | Antibacterial activity against novobiocin-resistant Streptococcus pneumoniae ATCC BAA-255 with GyrB S127L mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 0.5 ug ml-1 | Antibacterial activity against Enterococcus faecalis ATCC 29212 with GyrB T167A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 1 ug ml-1 | Antibacterial activity against Enterococcus faecalis ATCC 29212 after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 1 ug ml-1 | Antibacterial activity against Enterococcus faecalis ATCC 29212 with GyrB T167I mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 2 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 2 ug ml-1 | Antibacterial activity against novobiocin-resistant Haemophilus influenzae ATCC 51907 with GyrB R140C mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 2 ug ml-1 | Antibacterial activity against novobiocin-resistant Haemophilus influenzae ATCC 51907 with GyrB R140H mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 2 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 carrying plasmid expressing wild type GyrB | ChEMBL. | 17116675 |
MIC (functional) | = 2 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 carrying plasmid expressing GyrB R144I mutant | ChEMBL. | 17116675 |
MIC (functional) | = 2 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 without plasmid | ChEMBL. | 17116675 |
MIC (functional) | = 2 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 with GyrB R144I mutation without plasmid | ChEMBL. | 17116675 |
MIC (functional) | = 4 ug ml-1 | Antibacterial activity against novobiocin-resistant Staphylococcus aureus ATCC 29213 with GyrB R144I mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 4 ug ml-1 | Antibacterial activity against Streptococcus pneumoniae ATCC BAA-255 with ParE T172I mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 4 ug ml-1 | Antibacterial activity against Haemophilus influenzae ATCC 51907 after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 4 ug ml-1 | Antibacterial activity against novobiocin-resistant Haemophilus influenzae ATCC 51907 with GyrB R140L mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 8 ug ml-1 | Antibacterial activity against Streptococcus pneumoniae ATCC BAA-255 with ParE T172A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 8 ug ml-1 | Antibacterial activity against Enterococcus faecalis ATCC 29212 with ParE T169A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 8 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 carrying plasmid expressing GyrB T173N mutant | ChEMBL. | 17116675 |
MIC (functional) | = 8 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 carrying plasmid expressing GyrB T173I mutant | ChEMBL. | 17116675 |
MIC (functional) | = 8 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 with GyrB T173N mutation without plasmid | ChEMBL. | 17116675 |
MIC (functional) | = 8 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 with GyrB T173I mutation without plasmid | ChEMBL. | 17116675 |
MIC (functional) | = 16 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 with GyrB T173N mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 16 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 with GyrB T173I mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | > 64 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 with GyrB T173N and GrlB T166A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | > 64 ug ml-1 | Antibacterial activity against Staphylococcus aureus ATCC 29213 with GyrB T173I and GrlB T166A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | = 64 ug ml-1 | Antibacterial activity against Streptococcus pneumoniae ATCC BAA-255 with GyrB T172A and ParE T172A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | > 64 ug ml-1 | Antibacterial activity against Enterococcus faecalis ATCC 29212 with GyrB T167I and ParE T169A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | > 64 ug ml-1 | Antibacterial activity against Enterococcus faecalis ATCC 29212 with GyrB T167A and ParE T169A mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
MIC (functional) | > 64 ug ml-1 | Antibacterial activity against Haemophilus influenzae ATCC 51907 with GyrB T169I mutation after 18 to 20 hrs | ChEMBL. | 17116675 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.