Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Mus musculus | 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 | 358 aa | 361 aa | 33.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 4, putative | 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 | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0062 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0062 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Loa Loa (eye worm) | CMGC/MAPK/ERK1 protein kinase | 0.0062 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0062 | 0.5 | 0.5 |
Trypanosoma brucei | mitogen activated protein kinase 4, putative | 0.0062 | 0.5 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase 3 | 0.0062 | 0.5 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase 3 | 0.0062 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 2, putative | 0.0062 | 0.5 | 0.5 |
Trypanosoma brucei | protein kinase, putative | 0.0062 | 0.5 | 0.5 |
Leishmania major | mitogen activated protein kinase 4, putative;with=GeneDB:LmxM19.1440 | 0.0062 | 0.5 | 0.5 |
Leishmania major | mitogen activated protein kinase, putative,map kinase, putative | 0.0062 | 0.5 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase | 0.0062 | 0.5 | 0.5 |
Giardia lamblia | Kinase, CMGC MAPK | 0.0062 | 0.5 | 0.5 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0062 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 1.5 nM | BindingDB_Patents: IMAP-FP Assay. Condition 2: Activated ERK2 activity was determined in an IMAP-FP assay (Molecular Devices). Using this assay format, the potency (IC50) of each compound was determined from a 10 point (1:3 serial dilution, 3 uM starting compound concentration) titration curve using the following outlined procedure. 7.5 mL of compound (3333 fold dilution in final assay volume of 25 uL) was added to 15 uL of kinase buffer containing 0.0133 ng/mL (0.316 nM) of fully phosphorylated, mouse aERK2 enzyme. Following a 15 minute incubation, each reaction was initiated by the addition of 10 uL kinase buffer containing 2.45 uM ERK2 IMAP substrate peptides (2.25 uM-unlabeled IPTTPITTTYFFFK-COOH and 200 nM-labeled IPTTPITTTYFFFK-5FAM (5-carboxyfluorescein)-COOH), and 75 uM ATP. The final reaction in each well of 25 uL consists of 0.19 nM mouse ERK2, 900 nM unlabeled peptide, 80 nM labeled-peptide, and 30 uM ATP. Phosphorylation reactions were allowed to proceed for 40-45 minutes. | 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.