Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit beta | References | |
Homo sapiens | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha | References | |
Homo sapiens | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit delta | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Trypanosoma brucei | phosphatidylinositol 4-kinase alpha, putative | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit beta | 582 aa | 491 aa | 25.2 % |
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 |
---|---|---|---|---|
Trichomonas vaginalis | phopsphatidylinositol 3-kinase, drosophila, putative | 0.0611 | 0.0601 | 1 |
Entamoeba histolytica | phosphatidylinositol 3-kinase, putative | 0.0509 | 0.0476 | 0.7549 |
Loa Loa (eye worm) | hypothetical protein | 0.3499 | 0.4161 | 0.4123 |
Trypanosoma brucei | phosphatidylinositol 3-kinase, putative | 0.0197 | 0.0091 | 0.5 |
Schistosoma mansoni | aminopeptidase P homologue (M24 family) | 0.8236 | 1 | 1 |
Entamoeba histolytica | phosphatidylinositol 3-kinase, putative | 0.0251 | 0.0158 | 0.1307 |
Trypanosoma cruzi | phosphatidylinositol 3-kinase vps34-like | 0.0197 | 0.0091 | 0.0498 |
Trypanosoma cruzi | phosphatidylinositol 3-kinase 2, putative | 0.0611 | 0.0601 | 1 |
Echinococcus granulosus | bifunctional protein NCOAT | 0.8236 | 1 | 1 |
Trichomonas vaginalis | phosphatidylinositol kinase, putative | 0.0611 | 0.0601 | 1 |
Brugia malayi | Phosphatidylinositol 3- and 4-kinase family protein | 0.0353 | 0.0283 | 0.0193 |
Echinococcus multilocularis | bifunctional protein NCOAT | 0.8236 | 1 | 1 |
Giardia lamblia | Phosphoinositide-3-kinase, catalytic, alpha polypeptide | 0.0354 | 0.0284 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0258 | 0.0167 | 0.0103 |
Echinococcus granulosus | phosphatidylinositol 45 bisphosphate 3 kinase | 0.0923 | 0.0986 | 0.0724 |
Entamoeba histolytica | hypothetical protein | 0.0509 | 0.0476 | 0.7549 |
Trichomonas vaginalis | phosphatidylinositol 3-kinase catalytic subunit gamma, putative | 0.0611 | 0.0601 | 1 |
Brugia malayi | phosphoinositide 3'-hydroxykinase p110-alpha subunit, putative | 0.0312 | 0.0233 | 0.0144 |
Loa Loa (eye worm) | hypothetical protein | 0.0353 | 0.0283 | 0.022 |
Trypanosoma cruzi | phosphatidylinositol 3-kinase 2, putative | 0.0611 | 0.0601 | 1 |
Schistosoma mansoni | Hyaluronidase | 0.8236 | 1 | 1 |
Brugia malayi | Phosphatidylinositol 3- and 4-kinase family protein | 0.0611 | 0.0601 | 0.0515 |
Trichomonas vaginalis | phosphatidylinositol 3-kinase catalytic subunit alpha, beta, delta, putative | 0.0455 | 0.0409 | 0.6242 |
Entamoeba histolytica | phosphatidylinositol 3-kinase, putative | 0.0611 | 0.0601 | 1 |
Loa Loa (eye worm) | hyaluronidase | 0.8236 | 1 | 1 |
Loa Loa (eye worm) | phosphatidylinositol 3 | 0.0822 | 0.0861 | 0.0802 |
Trichomonas vaginalis | phosphatidylinositol 3-kinase class, putative | 0.0455 | 0.0409 | 0.6242 |
Schistosoma mansoni | phosphatidylinositol-45-bisphosphate 3-kinase catalytic subunit alpha PI3K | 0.0923 | 0.0986 | 0.0904 |
Entamoeba histolytica | phosphatidylinositol 3-kinase 1, putative | 0.0589 | 0.0574 | 0.9475 |
Echinococcus multilocularis | phosphatidylinositol 4,5 bisphosphate 3 kinase | 0.0923 | 0.0986 | 0.0724 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity | Toxicity in Harlan nude mouse xenografted with Rat1 cells expressing myr-p110alpha assessed as change in body weight at 25 to 50 mg/kg, po qd administered for 8 days measured during compound dosing | LITERATURE. | 27575470 | |
Activity | Toxicity in Harlan nude mouse xenografted with Rat1 cells expressing myr-p110alpha assessed as change in body weight at 100 mg/kg, po administered every second day from day 2 onwards for 8 days measured during compound dosing | LITERATURE. | 27575470 | |
Activity | = 11 % | Toxicity in Harlan nude mouse xenografted with Rat1 cells expressing myr-p110alpha assessed as reduction in body weight at 100 mg/kg, po qd administered for 8 days measured on day 4 | LITERATURE. | 27575470 |
IC50 (binding) | = 0.022 uM | Inhibition of PI3Kalpha (unknown origin) using L-a- phosphatidylinositol/OctylGlucoside as substrate after 10 mins by KinaseGlo luminescence assay | LITERATURE. | 27575470 |
IC50 (binding) | = 0.039 uM | Inhibition of PI3Kalpha (unknown origin) expressed in Rat1 cells assessed as reduction in Akt phosphorylation at Ser473 residue | LITERATURE. | 27575470 |
IC50 (binding) | = 1.53 uM | Inhibition of PI3Kdelta (unknown origin) expressed in Rat1 cells assessed as reduction in Akt phosphorylation at Ser473 residue | LITERATURE. | 27575470 |
IC50 (binding) | = 2.07 uM | Inhibition of PI3Kbeta (unknown origin) using L-a- phosphatidylinositol/OctylGlucoside as substrate after 10 mins by KinaseGlo luminescence assay | LITERATURE. | 27575470 |
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.
1 literature reference was collected for this gene.