Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | topoisomerase (DNA) I | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | pigment dispersing factor receptor c | 0.0049 | 0.0611 | 0.0802 |
Mycobacterium leprae | Probable fructose bisphosphate aldolase Fba | 0.014 | 0.421 | 0.5 |
Echinococcus multilocularis | DNA topoisomerase 1 | 0.0226 | 0.7619 | 1 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Toxoplasma gondii | DNA topoisomerase I, putative | 0.0226 | 0.7619 | 1 |
Schistosoma mansoni | DNA topoisomerase type I | 0.0226 | 0.7619 | 1 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Giardia lamblia | Fructose-bisphosphate aldolase | 0.0286 | 1 | 0.5 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Entamoeba histolytica | fructose-1,6-bisphosphate aldolase, putative | 0.0286 | 1 | 0.5 |
Brugia malayi | Choline/ethanolamine kinase family protein | 0.0164 | 0.5155 | 0.6766 |
Onchocerca volvulus | Heterochromatin protein 1 homolog | 0.0041 | 0.0308 | 1 |
Trypanosoma cruzi | DNA topoisomerase IB, large subunit, putative | 0.0169 | 0.5373 | 1 |
Trichomonas vaginalis | chromobox protein, putative | 0.0041 | 0.0308 | 0.0117 |
Schistosoma mansoni | DNA topoisomerase type I | 0.0169 | 0.5373 | 0.7052 |
Trypanosoma brucei | DNA topoisomerase IB, large subunit | 0.0169 | 0.5373 | 1 |
Trichomonas vaginalis | chromobox protein, putative | 0.0068 | 0.1379 | 0.1209 |
Brugia malayi | Calcitonin receptor-like protein seb-1 | 0.0049 | 0.0611 | 0.0802 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Brugia malayi | Corticotropin releasing factor receptor 2 precursor, putative | 0.0049 | 0.0611 | 0.0802 |
Mycobacterium tuberculosis | Probable fructose-bisphosphate aldolase Fba | 0.014 | 0.421 | 0.5 |
Loa Loa (eye worm) | heterochromatin protein 1 | 0.0068 | 0.1379 | 0.1809 |
Plasmodium falciparum | topoisomerase I | 0.0226 | 0.7619 | 1 |
Brugia malayi | chromobox protein homolog 3 | 0.0038 | 0.0193 | 0.0253 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Leishmania major | DNA topoisomerase IB, large subunit | 0.0169 | 0.5373 | 1 |
Brugia malayi | Heterochromatin protein 1 | 0.0068 | 0.1379 | 0.1809 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0038 | 0.0193 | 0.0253 |
Loa Loa (eye worm) | DNA topoisomerase I | 0.0226 | 0.7619 | 1 |
Trichomonas vaginalis | chromobox protein, putative | 0.0041 | 0.0308 | 0.0117 |
Trichomonas vaginalis | fructose-bisphosphate aldolase, putative | 0.0286 | 1 | 1 |
Echinococcus granulosus | choline:ethanolamine kinase | 0.0164 | 0.5155 | 0.6051 |
Mycobacterium ulcerans | fructose-bisphosphate aldolase | 0.014 | 0.421 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0049 | 0.0611 | 0.0802 |
Schistosoma mansoni | DNA topoisomerase type I | 0.0169 | 0.5373 | 0.7052 |
Schistosoma mansoni | chromobox protein | 0.0068 | 0.1379 | 0.1809 |
Echinococcus granulosus | DNA topoisomerase 1 | 0.0226 | 0.7619 | 1 |
Schistosoma mansoni | chromobox protein | 0.0068 | 0.1379 | 0.1809 |
Echinococcus multilocularis | choline:ethanolamine kinase | 0.0164 | 0.5155 | 0.6051 |
Plasmodium vivax | topoisomerase I, putative | 0.0226 | 0.7619 | 1 |
Treponema pallidum | fructose-bisphosphate aldolase | 0.0286 | 1 | 0.5 |
Loa Loa (eye worm) | choline/ethanolamine kinase | 0.0164 | 0.5155 | 0.6766 |
Brugia malayi | DNA topoisomerase I | 0.0226 | 0.7619 | 1 |
Trichomonas vaginalis | chromobox protein, putative | 0.0068 | 0.1379 | 0.1209 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC200 (functional) | = 0.65 uM | Inhibition of protein-DNA complex in P388 (murine leukaemia) cells. | ChEMBL. | 10612590 |
EC200 (functional) | = 0.65 uM | Inhibition of protein-DNA complex in P388 (murine leukaemia) cells. | ChEMBL. | 10612590 |
EC50 (binding) | = 0.055 uM | In vitro inhibition of Topoisomerase I-mediated DNA cleavage using supercoiled pBR322 plasmid DNA. | ChEMBL. | 10612590 |
EC50 (binding) | = 0.055 uM | In vitro inhibition of Topoisomerase I-mediated DNA cleavage using supercoiled pBR322 plasmid DNA. | ChEMBL. | 10612590 |
EC50 (binding) | > 50 uM | In vitro inhibition of Topoisomerase II-mediated DNA cleavage using supercoiled pBR322 plasmid DNA. | ChEMBL. | 10612590 |
EC50 (binding) | > 50 uM | In vitro inhibition of Topoisomerase II-mediated DNA cleavage using supercoiled pBR322 plasmid DNA. | ChEMBL. | 10612590 |
GID75 (functional) | = 710 mg m**-2 | Tested for anticancer effect on MKN-45 human stomach cancer cells implanted subcutaneously into flanks of nude mice. | ChEMBL. | 10612590 |
GID75 (functional) | = 710 mg m**-2 | Tested for anticancer effect on MKN-45 human stomach cancer cells implanted subcutaneously into flanks of nude mice. | ChEMBL. | 10612590 |
IC50 (functional) | = 3.5 nM | In vitro cytotoxicity against p388 (murine leukaemia) cells. | ChEMBL. | 10612590 |
IC50 (functional) | = 3.5 nM | In vitro cytotoxicity against p388 (murine leukaemia) cells. | ChEMBL. | 10612590 |
IC50 (functional) | = 120 nM | In vitro cytotoxicity against MKN-45 (human stomach cancer) cells. | ChEMBL. | 10612590 |
IC50 (functional) | = 120 nM | In vitro cytotoxicity against MKN-45 (human stomach cancer) cells. | ChEMBL. | 10612590 |
IC50 (functional) | = 340 nM | In vitro cytotoxicity against DLD-1 (human colon cancer) cells. | ChEMBL. | 10612590 |
IC50 (functional) | = 340 nM | In vitro cytotoxicity against DLD-1 (human colon cancer) cells. | ChEMBL. | 10612590 |
IC50 (functional) | = 90 uM | In vitro inhibition of PKC mediated DNA cleavage. | ChEMBL. | 10612590 |
IC50 (functional) | = 90 uM | In vitro inhibition of PKC mediated DNA cleavage. | ChEMBL. | 10612590 |
LD10 (functional) | = 1000 mg m**-2 | Tested for anticancer effect on MKN-45 human stomach cancer cells implanted subcutaneously into flanks of nude mice. | ChEMBL. | 10612590 |
LD10 (functional) | = 1000 mg m**-2 | Tested for anticancer effect on MKN-45 human stomach cancer cells implanted subcutaneously into flanks of nude mice. | ChEMBL. | 10612590 |
Ratio (functional) | = 1.4 | Compound was tested for anticancer effect on cancer cells implanted subcutaneously into flanks of nude mice and safety margin was determined (LD10/GID75) | ChEMBL. | 10612590 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 10612590 | |
Mus musculus | ChEMBL23 | 10612590 |
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.