Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Plasmodium falciparum | plasmepsin II | No references | |
Plasmodium falciparum | plasmepsin IV | No references | |
Homo sapiens | beta-site APP-cleaving enzyme 1 | No references | |
Homo sapiens | cathepsin E | No references | |
Homo sapiens | cathepsin D | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Plasmodium falciparum | plasmepsin X | cathepsin E | 396 aa | 340 aa | 32.1 % |
Plasmodium falciparum | plasmepsin VII | beta-site APP-cleaving enzyme 1 | 401 aa | 352 aa | 21.3 % |
Plasmodium falciparum | plasmepsin X | cathepsin D | 412 aa | 339 aa | 28.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trichomonas vaginalis | CMGC family protein kinase | 0.1865 | 1 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 4, putative | 0.1865 | 1 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.1865 | 1 | 0.5 |
Toxoplasma gondii | CMGC kinase, MAPK family (ERK) MAPK-1 | 0.1865 | 1 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 2, putative | 0.1865 | 1 | 0.5 |
Leishmania major | mitogen activated protein kinase 4, putative;with=GeneDB:LmxM19.1440 | 0.1865 | 1 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.1865 | 1 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.1865 | 1 | 0.5 |
Loa Loa (eye worm) | CMGC/MAPK/ERK1 protein kinase | 0.1865 | 1 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.1865 | 1 | 0.5 |
Trypanosoma brucei | mitogen activated protein kinase 4, putative | 0.1865 | 1 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase 3 | 0.1865 | 1 | 0.5 |
Schistosoma mansoni | memapsin-2 (A01 family) | 0.0591 | 0.034 | 0.034 |
Echinococcus granulosus | mitogen activated protein kinase 3 | 0.1865 | 1 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.1865 | 1 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase | 0.1865 | 1 | 0.5 |
Trypanosoma brucei | protein kinase, putative | 0.1865 | 1 | 0.5 |
Leishmania major | mitogen activated protein kinase, putative,map kinase, putative | 0.1865 | 1 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase | 0.1865 | 1 | 0.5 |
Giardia lamblia | Kinase, CMGC MAPK | 0.1865 | 1 | 0.5 |
Schistosoma mansoni | serine/threonine protein kinase | 0.1865 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Cp (ADMET) | = 4140 ng/ml | Plasma concentration in Plasmodium chabaudi ASS infected NIH mouse at 110 mg/kg, po qd measured 30 mins after post last dose on day 3 | ChEMBL. | 24900778 |
IC50 (binding) | = 6.81 nM | Enzyme Inhibition Assay | BINDINGDB. | No reference |
IC50 (binding) | = 7 nM | Enzyme Inhibition Assay | BINDINGDB. | No reference |
IC50 (binding) | = 18 nM | Enzyme Inhibition Assay | BINDINGDB. | No reference |
IC50 (binding) | = 511 nM | Fluorescence Resonance Energy Transfer (FRET) Assay | BINDINGDB. | No reference |
IC50 (binding) | > 10000 nM | Fluorescence Resonance Energy Transfer (FRET) Assay | BINDINGDB. | No reference |
IC50 (binding) | = 10000 nM | Fluorescence Resonance Energy Transfer (FRET) Assay | BINDINGDB. | No reference |
IC50 (binding) | = 10100 nM | Fluorescence Resonance Energy Transfer (FRET) Assay | BINDINGDB. | No reference |
IC50 (functional) | = 0.459 uM | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in RBV after 72 hrs by SYBR Green I-based fluorescence method | ChEMBL. | 24900778 |
Inhibition (ADMET) | Inhibition of human recombinant CYP2C19 after 30 mins | ChEMBL. | 24900778 | |
Inhibition (ADMET) | Inhibition of human recombinant CYP3A4 after 30 mins | ChEMBL. | 24900778 | |
Inhibition (ADMET) | Inhibition of human recombinant CYP2D6 after 30 mins | ChEMBL. | 24900778 | |
Inhibition (functional) | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in RBV after 48 hrs by SYBR Green I-based fluorescence method | ChEMBL. | 24900778 | |
Inhibition (ADMET) | Inhibition of human recombinant CYP1A2 after 30 mins | ChEMBL. | 24900778 | |
Inhibition (ADMET) | Inhibition of human recombinant CYP2C9 after 30 mins | ChEMBL. | 24900778 | |
Inhibition (functional) | = 63 % | Antimalarial activity against Plasmodium chabaudi ASS infected in NIH mouse assessed as inhibition of parasitemia at 110 mg/kg, po qd for 4 days | ChEMBL. | 24900778 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Plasmodium falciparum | 24900778 |
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.