Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | MDM2 proto-oncogene, E3 ubiquitin protein ligase | Starlite/ChEMBL | No references |
Homo sapiens | MDM4, p53 regulator | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | thymidylate synthase | 0.0291 | 1 | 1 |
Chlamydia trachomatis | SWIB complex protein | 0.0026 | 0 | 0.5 |
Trypanosoma cruzi | dihydrofolate reductase-thymidylate synthase | 0.0291 | 1 | 1 |
Leishmania major | dihydrofolate reductase-thymidylate synthase | 0.0291 | 1 | 0.5 |
Schistosoma mansoni | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0291 | 1 | 1 |
Mycobacterium leprae | PROBABLE THYMIDYLATE SYNTHASE THYA (TS) (TSASE) | 0.0291 | 1 | 0.5 |
Mycobacterium tuberculosis | Probable thymidylate synthase ThyA (ts) (TSASE) | 0.0291 | 1 | 1 |
Echinococcus granulosus | thymidylate synthase | 0.0291 | 1 | 1 |
Trypanosoma brucei | dihydrofolate reductase-thymidylate synthase | 0.0291 | 1 | 0.5 |
Mycobacterium ulcerans | thymidylate synthase | 0.0291 | 1 | 0.5 |
Plasmodium vivax | bifunctional dihydrofolate reductase-thymidylate synthase, putative | 0.0291 | 1 | 1 |
Brugia malayi | hypothetical protein | 0.0138 | 0.4245 | 0.4245 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0138 | 0.4245 | 1 |
Onchocerca volvulus | 0.0291 | 1 | 1 | |
Chlamydia trachomatis | DNA topoisomerase I | 0.0026 | 0 | 0.5 |
Plasmodium falciparum | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0291 | 1 | 1 |
Echinococcus multilocularis | thymidylate synthase | 0.0291 | 1 | 1 |
Toxoplasma gondii | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0291 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 8010 nM | BindingDB_Patents: Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay. The inhibition of p53-Hdm2 and p53-Hdm4 interactions is measured by time resolved fluorescence energy transfer (TR-FRET). Fluorescence energy transfer (or Foerster resonance energy transfer) describes an energy transfer between donor and acceptor fluorescent molecules. For this assay, MDM2 protein (amino acids 2-188) and MDM4 protein (amino acids 2-185), tagged with a C-terminal Biotin moiety, are used in combination with a Europium labeled streptavidin (Perkin Elmer, Inc., Waltham, Mass., USA) serving as the donor fluorophore. The p53 derived, Cy5 labeled peptide Cy5-TFSDLWKLL (p53 aa 18-26) is the energy acceptor. Upon excitation of the donor molecule at 340 nm, binding interaction between MDM2 or MDM4 and the p53 peptide induces energy transfer and enhanced response at the acceptor emission wavelength at 665 nm. Disruption of the formation of the p53-MDM2 or p53-MDM4 complex due to an inhibitor molecule binding to the p53 binding site of MDM2 or MDM4 results in increased donor emission. | 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.