Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | mitogen-activated protein kinase 1 | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Trypanosoma brucei | mitogen-activated protein kinase 5 | mitogen-activated protein kinase 1 | 360 aa | 361 aa | 33.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase | 0.0062 | 0.5 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase 3 | 0.0062 | 0.5 | 0.5 |
Leishmania major | mitogen activated protein kinase 4, putative;with=GeneDB:LmxM19.1440 | 0.0062 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0062 | 0.5 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase | 0.0062 | 0.5 | 0.5 |
Trypanosoma brucei | protein kinase, putative | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 4, putative | 0.0062 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Toxoplasma gondii | CMGC kinase, MAPK family (ERK) MAPK-1 | 0.0062 | 0.5 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase 3 | 0.0062 | 0.5 | 0.5 |
Giardia lamblia | Kinase, CMGC MAPK | 0.0062 | 0.5 | 0.5 |
Trypanosoma brucei | mitogen activated protein kinase 4, putative | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0062 | 0.5 | 0.5 |
Leishmania major | mitogen activated protein kinase, putative,map kinase, putative | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 2, putative | 0.0062 | 0.5 | 0.5 |
Loa Loa (eye worm) | CMGC/MAPK/ERK1 protein kinase | 0.0062 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 4 nM | BindingDB_Patents: Cell-Free Kinase Assays. The inhibitory effect of the compounds according to the invention was tested on various serine/threonine, tyrosine and lipid kinases in enzymatic assays. Recombinant human kinases such as, for example, Erk2, were used in this case, partly as full-length kinases, partly as shortened fragments, but at least consisting of the functional kinase domains. The commercial kinase proteins (Proqinase, Upstate) were used as recombinant fusion proteins with GST (glutathion-S-transferase) or His-Tag. Depending on the type of substrate, the various kinase reactions were quantified by means of suitable ALPHA beads (Perkin-Elmer). MAPK-ALPHAs (e.g. Erk2): the test substance, 0.625 ng Erk2 (#14-173, Upstate), 10 uM ATP and 15 nM biotinylated MBP (myelin basic protein) substrate were incubated on a 384-well Optiplate (Perkin-Elmer) in a volume of 15 ul for 1 h in 25 mM Tris, 10 mM MgCl2, 0.1% Tween-20, 100 uM NaVO4, 2 mM DTT at pH 7.5. | 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.