Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | pyruvate kinase, muscle | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | pyruvate kinase | pyruvate kinase, muscle | 605 aa | 521 aa | 34.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Pyruvate kinase, M2 isozyme | 0.004 | 0.0887 | 0.0887 |
Echinococcus multilocularis | pyruvate kinase | 0.004 | 0.0887 | 0.2118 |
Trichomonas vaginalis | dihydroorotate dehydrogenase, putative | 0.0136 | 0.3719 | 1 |
Entamoeba histolytica | dihydropyrimidine dehydrogenase, putative | 0.0136 | 0.3719 | 1 |
Brugia malayi | Dihydroorotate dehydrogenase, mitochondrial precursor, putative | 0.0348 | 1 | 1 |
Trypanosoma brucei | dihydroorotate dehydrogenase (fumarate) | 0.0348 | 1 | 1 |
Echinococcus granulosus | muscleblind protein | 0.0152 | 0.419 | 1 |
Echinococcus multilocularis | pyruvate kinase | 0.0021 | 0.0307 | 0.0734 |
Onchocerca volvulus | Pyruvate kinase homolog | 0.004 | 0.0887 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0152 | 0.419 | 1 |
Loa Loa (eye worm) | pyruvate kinase | 0.004 | 0.0887 | 0.2118 |
Mycobacterium ulcerans | aldehyde dehydrogenase | 0.0062 | 0.1523 | 0.0697 |
Toxoplasma gondii | dihydroorotate dehydrogenase reveal, putative | 0.0348 | 1 | 1 |
Plasmodium falciparum | pyruvate kinase | 0.004 | 0.0887 | 0.0598 |
Brugia malayi | Pyruvate kinase, alpha/beta domain containing protein | 0.0012 | 0.0056 | 0.0056 |
Echinococcus multilocularis | dihydropyrimidine dehydrogenase (NADP+) | 0.0136 | 0.3719 | 0.8876 |
Brugia malayi | Zinc finger, C2H2 type family protein | 0.0136 | 0.3719 | 0.3719 |
Giardia lamblia | Pyruvate kinase | 0.004 | 0.0887 | 1 |
Trichomonas vaginalis | dihydropyrimidine dehydrogenase, putative | 0.0136 | 0.3719 | 1 |
Brugia malayi | Muscleblind-like protein | 0.0152 | 0.419 | 0.419 |
Schistosoma mansoni | pyruvate kinase | 0.004 | 0.0887 | 0.0887 |
Loa Loa (eye worm) | hypothetical protein | 0.0152 | 0.419 | 1 |
Echinococcus granulosus | pyruvate kinase | 0.0021 | 0.0307 | 0.0734 |
Mycobacterium ulcerans | aldehyde dehydrogenase | 0.0062 | 0.1523 | 0.0697 |
Mycobacterium leprae | Probable dihydroorotate dehydrogenase PyrD | 0.0348 | 1 | 1 |
Echinococcus granulosus | pyruvate kinase | 0.0021 | 0.0307 | 0.0734 |
Echinococcus granulosus | aldehyde dehydrogenase mitochondrial | 0.0062 | 0.1523 | 0.3634 |
Echinococcus granulosus | pyruvate kinase | 0.004 | 0.0887 | 0.2118 |
Echinococcus granulosus | dihydropyrimidine dehydrogenase NADP | 0.0136 | 0.3719 | 0.8876 |
Plasmodium falciparum | dihydroorotate dehydrogenase | 0.0348 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.0887 | 0.2118 |
Trypanosoma cruzi | dihydroorotate dehydrogenase, putative | 0.0348 | 1 | 1 |
Loa Loa (eye worm) | pyruvate kinase | 0.004 | 0.0887 | 0.2118 |
Loa Loa (eye worm) | pyruvate kinase-PB | 0.0028 | 0.0527 | 0.1257 |
Echinococcus granulosus | pyruvate kinase | 0.004 | 0.0887 | 0.2118 |
Onchocerca volvulus | Pyruvate kinase homolog | 0.004 | 0.0887 | 1 |
Schistosoma mansoni | dihydroorotate dehydrogenase | 0.0348 | 1 | 1 |
Echinococcus multilocularis | pyruvate kinase | 0.0021 | 0.0307 | 0.0734 |
Echinococcus granulosus | pyruvate kinase | 0.0021 | 0.0307 | 0.0734 |
Echinococcus multilocularis | aldehyde dehydrogenase, mitochondrial | 0.0062 | 0.1523 | 0.3634 |
Mycobacterium tuberculosis | Probable dihydroorotate dehydrogenase PyrD | 0.0348 | 1 | 1 |
Trichomonas vaginalis | dihydroorotate dehydrogenase, putative | 0.0136 | 0.3719 | 1 |
Schistosoma mansoni | aldehyde dehydrogenase | 0.0062 | 0.1523 | 0.1523 |
Mycobacterium tuberculosis | Probable aldehyde dehydrogenase | 0.0062 | 0.1523 | 0.0697 |
Echinococcus multilocularis | pyruvate kinase | 0.0032 | 0.0636 | 0.1519 |
Loa Loa (eye worm) | pyruvate kinase | 0.004 | 0.0887 | 0.2118 |
Plasmodium vivax | pyruvate kinase, putative | 0.004 | 0.0887 | 0.0598 |
Toxoplasma gondii | aldehyde dehydrogenase | 0.0062 | 0.1523 | 0.1254 |
Trypanosoma cruzi | dihydroorotate dehydrogenase, putative | 0.0348 | 1 | 1 |
Trypanosoma cruzi | dihydroorotate dehydrogenase, putative | 0.0136 | 0.3719 | 0.3108 |
Echinococcus multilocularis | dihydropyrimidine dehydrogenase (NADP+) | 0.0136 | 0.3719 | 0.8876 |
Mycobacterium ulcerans | dihydroorotate dehydrogenase 2 | 0.0348 | 1 | 1 |
Plasmodium vivax | dihydroorotate dehydrogenase, mitochondrial precursor, putative | 0.0348 | 1 | 1 |
Mycobacterium ulcerans | aldehyde dehydrogenase | 0.0062 | 0.1523 | 0.0697 |
Onchocerca volvulus | Pyruvate kinase homolog | 0.004 | 0.0887 | 1 |
Echinococcus multilocularis | pyruvate kinase | 0.004 | 0.0887 | 0.2118 |
Chlamydia trachomatis | pyruvate kinase | 0.004 | 0.0887 | 0.5 |
Brugia malayi | Pyruvate kinase, muscle isozyme | 0.004 | 0.0887 | 0.0887 |
Echinococcus multilocularis | muscleblind protein 1 | 0.0152 | 0.419 | 1 |
Schistosoma mansoni | aldehyde dehydrogenase | 0.0062 | 0.1523 | 0.1523 |
Wolbachia endosymbiont of Brugia malayi | dihydroorotate dehydrogenase 2 | 0.0348 | 1 | 0.5 |
Trichomonas vaginalis | dihydroorotate dehydrogenase, putative | 0.0136 | 0.3719 | 1 |
Echinococcus multilocularis | pyruvate kinase | 0.0021 | 0.0307 | 0.0734 |
Trichomonas vaginalis | dihydroorotate dehydrogenase, putative | 0.0136 | 0.3719 | 1 |
Schistosoma mansoni | pyruvate kinase | 0.004 | 0.0887 | 0.0887 |
Echinococcus granulosus | dihydropyrimidine dehydrogenase NADP | 0.0136 | 0.3719 | 0.8876 |
Leishmania major | dihydroorotate dehydrogenase | 0.0348 | 1 | 1 |
Echinococcus multilocularis | muscleblind protein | 0.0152 | 0.419 | 1 |
Trichomonas vaginalis | dihydroorotate dehydrogenase, putative | 0.0136 | 0.3719 | 1 |
Trypanosoma cruzi | dihydroorotate dehydrogenase (fumarate), putative | 0.0348 | 1 | 1 |
Toxoplasma gondii | pyruvate kinase PyK1 | 0.004 | 0.0887 | 0.0598 |
Leishmania major | aldehyde dehydrogenase, mitochondrial precursor | 0.0062 | 0.1523 | 0.0697 |
Schistosoma mansoni | pyruvate kinase | 0.0021 | 0.0307 | 0.0307 |
Loa Loa (eye worm) | hypothetical protein | 0.0028 | 0.0527 | 0.1257 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | = 0.07 uM | Activation of human PKM2 assessed as ATP product formation after 1 hr by luminescent pyruvate kinase-luciferase coupled assay | ChEMBL. | 21958545 |
Emax (binding) | = 92 % | Activation of human PKM2 assessed as ATP product formation at 57 mM after 1 hr by luminescent pyruvate kinase-luciferase coupled assay | ChEMBL. | 21958545 |
Potency (functional) | 0.1634 uM | PUBCHEM_BIOASSAY: Confirmation Concentration-Response Assay for Activators of Human Muscle isoform 2 Pyruvate Kinase: for Probe SAR. (Class of assay: confirmatory) | ChEMBL. | No reference |
Potency (functional) | 0.4606 uM | PUBCHEM_BIOASSAY: Secondary LDH Assay for Activators of Human Pyruvate Kinase M2 isoform: for Probe SAR. (Class of assay: confirmatory) | ChEMBL. | No reference |
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.