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 |
---|---|---|---|---|
Schistosoma mansoni | brg-1 associated factor | 0.0026 | 0.5 | 0.5 |
Chlamydia trachomatis | SWIB complex protein | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | Upstream activation factor subunit UAF30 | 0.0026 | 0.5 | 0.5 |
Plasmodium falciparum | SWIB/MDM2 domain-containing protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Brugia malayi | brahma associated protein 60 kDa | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | Upstream activation factor subunit UAF30 | 0.0026 | 0.5 | 0.5 |
Toxoplasma gondii | SWIB/MDM2 domain-containing protein | 0.0026 | 0.5 | 0.5 |
Plasmodium falciparum | SWIB/MDM2 domain-containing protein | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | brahma associated protein | 0.0026 | 0.5 | 0.5 |
Toxoplasma gondii | DNA topoisomerase domain-containing protein | 0.0026 | 0.5 | 0.5 |
Plasmodium vivax | SWIB/MDM2 domain-containing protein, putative | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | SWI:SNF matrix associated | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | SWI:SNF matrix associated | 0.0026 | 0.5 | 0.5 |
Plasmodium vivax | hypothetical protein, conserved | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | SWIB/MDM2 domain-containing protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | SWI:SNF matrix associated | 0.0026 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0026 | 0.5 | 0.5 | |
Echinococcus granulosus | SWI:SNF matrix associated | 0.0026 | 0.5 | 0.5 |
Chlamydia trachomatis | DNA topoisomerase I | 0.0026 | 0.5 | 0.5 |
Brugia malayi | SWIB/MDM2 domain containing protein | 0.0026 | 0.5 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0026 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 4130 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.