Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Entamoeba histolytica | phosphatidylinositol 3-kinase, putative | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha | 1068 aa | 927 aa | 29.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trypanosoma cruzi | phosphatidylinositol 3-kinase 2, putative | 0.0118 | 0.0376 | 1 |
Trichomonas vaginalis | phosphatidylinositol 3-kinase catalytic subunit alpha, beta, delta, putative | 0.0081 | 0.0199 | 0.5294 |
Echinococcus multilocularis | phosphatidylinositol 4,5 bisphosphate 3 kinase | 0.0222 | 0.0873 | 0.0709 |
Loa Loa (eye worm) | phosphatidylinositol 3 | 0.0198 | 0.0758 | 0.665 |
Brugia malayi | phosphoinositide 3'-hydroxykinase p110-alpha subunit, putative | 0.0104 | 0.0309 | 0.2719 |
Schistosoma mansoni | kinesin eg-5 | 0.0277 | 0.1135 | 0.1308 |
Entamoeba histolytica | hypothetical protein | 0.0094 | 0.0261 | 0.2296 |
Entamoeba histolytica | kinesin, putative | 0.0277 | 0.1135 | 1 |
Trichomonas vaginalis | phosphatidylinositol 3-kinase catalytic subunit gamma, putative | 0.0118 | 0.0376 | 1 |
Trypanosoma cruzi | phosphatidylinositol 3-kinase 2, putative | 0.0118 | 0.0376 | 1 |
Trichomonas vaginalis | phosphatidylinositol 3-kinase class, putative | 0.0081 | 0.0199 | 0.5294 |
Entamoeba histolytica | phosphatidylinositol 3-kinase 1, putative | 0.0115 | 0.0359 | 0.3165 |
Entamoeba histolytica | phosphatidylinositol 3-kinase, putative | 0.0094 | 0.0261 | 0.2296 |
Loa Loa (eye worm) | kinesin-like protein KLP2 | 0.0277 | 0.1135 | 1 |
Schistosoma mansoni | phosphatidylinositol-45-bisphosphate 3-kinase catalytic subunit alpha PI3K | 0.0222 | 0.0873 | 0.1007 |
Echinococcus multilocularis | kinesin family 1 | 0.2134 | 1 | 1 |
Trypanosoma brucei | phosphatidylinositol 3-kinase, putative | 0.004 | 0 | 0.5 |
Entamoeba histolytica | phosphatidylinositol 3-kinase, putative | 0.0052 | 0.0062 | 0.0542 |
Plasmodium falciparum | kinesin-5 | 0.0277 | 0.1135 | 0.5 |
Giardia lamblia | Kinesin-5 | 0.0277 | 0.1135 | 1 |
Schistosoma mansoni | hypothetical protein | 0.1856 | 0.8676 | 1 |
Brugia malayi | Phosphatidylinositol 3- and 4-kinase family protein | 0.0118 | 0.0376 | 0.3312 |
Plasmodium vivax | kinesin-5 | 0.0277 | 0.1135 | 0.5 |
Brugia malayi | Phosphatidylinositol 3- and 4-kinase family protein | 0.0077 | 0.0177 | 0.1559 |
Trichomonas vaginalis | phopsphatidylinositol 3-kinase, drosophila, putative | 0.0118 | 0.0376 | 1 |
Entamoeba histolytica | phosphatidylinositol 3-kinase, putative | 0.0118 | 0.0376 | 0.3312 |
Toxoplasma gondii | kinesin motor domain-containing protein | 0.0277 | 0.1135 | 0.5 |
Trichomonas vaginalis | phosphatidylinositol kinase, putative | 0.0118 | 0.0376 | 1 |
Brugia malayi | Kinesin motor domain containing protein | 0.0277 | 0.1135 | 1 |
Echinococcus granulosus | phosphatidylinositol 45 bisphosphate 3 kinase | 0.0222 | 0.0873 | 0.0709 |
Loa Loa (eye worm) | hypothetical protein | 0.0077 | 0.0177 | 0.1483 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 108 nM | BindingDB_Patents: Biological Assays. The efficacy of compounds of the invention in inhibiting the PI3K induced-lipid phosphorylation may be tested in the following binding assay. The assay combines the scintillation proximity assay technology (SPA, Amersham) with the capacity of neomycin (a polycationic antibiotic) to bind phospholipids with high affinity and specificity. The Scintillation Proximity Assay is based on the properties of weakly emitting isotopes (such as 3H, 125I, 33P). Coating SPA beads with neomycin allows the detection of phosphorylated lipid substrates after incubation with recombinant PI3K and radioactive ATP in the same well, by capturing the radioactive phospholipids to the SPA beads through their specific binding to neomycin. | 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.