Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | p21 protein (Cdc42/Rac)-activated kinase 2 | References | |
Homo sapiens | p21 protein (Cdc42/Rac)-activated kinase 1 | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trichomonas vaginalis | STE family protein kinase | 0.009 | 1 | 1 |
Trichomonas vaginalis | STE family protein kinase | 0.009 | 1 | 1 |
Loa Loa (eye worm) | STE/STE20/PAKA protein kinase | 0.0053 | 0.2768 | 0.2808 |
Giardia lamblia | Kinase, STE STE20 | 0.009 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.009 | 0.9857 | 1 |
Echinococcus granulosus | p21 activated protein kinase 1 Dpak1 | 0.009 | 1 | 1 |
Echinococcus multilocularis | p21 activated protein kinase 1 Dpak1 | 0.009 | 1 | 1 |
Schistosoma mansoni | protein kinase | 0.009 | 1 | 1 |
Echinococcus multilocularis | serine:threonine protein kinase PAK 3 | 0.009 | 1 | 1 |
Trypanosoma cruzi | STE/STE20 serine/threonine-protein kinase, putative | 0.0053 | 0.2768 | 0.5 |
Echinococcus granulosus | serine:threonine protein kinase PAK 3 | 0.009 | 1 | 1 |
Trichomonas vaginalis | STE family protein kinase | 0.009 | 1 | 1 |
Trypanosoma cruzi | p21-activated kinase 3, putative | 0.0053 | 0.2768 | 0.5 |
Trichomonas vaginalis | STE family protein kinase | 0.009 | 1 | 1 |
Echinococcus granulosus | serine:threonine protein kinase PAK 3 | 0.009 | 1 | 1 |
Brugia malayi | p21/Cdc42/Rac1-activated kinase | 0.0053 | 0.2768 | 0.2768 |
Schistosoma mansoni | protein kinase | 0.009 | 1 | 1 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0053 | 0.2768 | 0.2768 |
Entamoeba histolytica | protein kinase, putative | 0.009 | 1 | 1 |
Echinococcus multilocularis | serine:threonine protein kinase PAK 3 | 0.009 | 1 | 1 |
Entamoeba histolytica | p21-activated kinase | 0.009 | 1 | 1 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0053 | 0.2768 | 0.2768 |
Loa Loa (eye worm) | STE/STE20/PAKA protein kinase | 0.0053 | 0.2768 | 0.2808 |
Trichomonas vaginalis | mitogen-activated protein kinase kinase kinase 3, MAPKKK3, MEKK3, putative | 0.0053 | 0.2768 | 0.2768 |
Trichomonas vaginalis | conserved hypothetical protein | 0.009 | 0.9857 | 0.9857 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (ADMET) | Toxicity in mouse at 100 mg/kg, ip | ChEMBL. | 27167326 | |
Cmax (ADMET) | = 28 uM | Cmax associated with acute adverse effect in mouse at 100 mg/kg, ip | ChEMBL. | 27167326 |
fCmax (ADMET) | = 0.76 uM | fCmax associated with acute adverse effect in mouse at 100 mg/kg, ip | ChEMBL. | 27167326 |
IC50 (binding) | = 0.24 uM | Inhibition of PAK1/2 in human EBC1 cells assessed as phosphorylation of MEK1 at serine 298 after 2 hrs by HTRF assay | ChEMBL. | 27167326 |
Ki (binding) | = 9.5 nM | Inhibition of human recombinant PAK2 assessed as phosphorylation of coumarin labeled FRET peptide substrate at Ser/Thr19 preincubated for 10 mins followed by ATP addition measured after 60 mins by Z'-LYTE assay | ChEMBL. | 27167326 |
Ki (binding) | = 11 nM | Inhibition of human recombinant N-terminal 6-His-tagged PAK1 kinase domain (249 to 545 residues) expressed in Escherichia coli BL21(DE3) assessed as phosphorylation of coumarin labeled FRET peptide substrate at Ser/Thr19 preincubated for 10 mins followed by ATP addition measured after 60 mins by Z'-LYTE assay | ChEMBL. | 27167326 |
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.