Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | p21 protein (Cdc42/Rac)-activated kinase 4 | Starlite/ChEMBL | References |
Homo sapiens | p21 protein (Cdc42/Rac)-activated kinase 1 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | serine/threonine protein kinase | 0.0069 | 0.1539 | 1 |
Entamoeba histolytica | serine/threonine protein kinase 6, putative | 0.0069 | 0.1539 | 1 |
Trypanosoma brucei | aurora B kinase | 0.0069 | 0.1539 | 0.5 |
Entamoeba histolytica | protein kinase, putative | 0.0039 | 0.0064 | 0.0416 |
Echinococcus granulosus | serine:threonine protein kinase PAK 3 | 0.0065 | 0.1349 | 0.1656 |
Echinococcus granulosus | p21 activated protein kinase 1 Dpak1 | 0.0065 | 0.1349 | 0.1656 |
Trichomonas vaginalis | STE family protein kinase | 0.0065 | 0.1349 | 0.8711 |
Trichomonas vaginalis | AGC family protein kinase | 0.0069 | 0.1539 | 1 |
Echinococcus multilocularis | p21 activated protein kinase 1 Dpak1 | 0.0065 | 0.1349 | 0.1656 |
Plasmodium falciparum | serine/threonine protein kinase, putative | 0.0069 | 0.1539 | 0.5 |
Leishmania major | protein kinase, putative | 0.0069 | 0.1539 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0064 | 0.1284 | 0.1284 |
Trichomonas vaginalis | STE family protein kinase | 0.0065 | 0.1349 | 0.8711 |
Brugia malayi | Protein kinase domain | 0.0065 | 0.1349 | 0.1349 |
Loa Loa (eye worm) | AUR protein kinase | 0.0069 | 0.1539 | 0.1539 |
Echinococcus multilocularis | PAK box P21 Rho binding | 0.0039 | 0.0064 | 0.0079 |
Trichomonas vaginalis | STE family protein kinase | 0.0065 | 0.1349 | 0.8711 |
Loa Loa (eye worm) | AUR protein kinase | 0.0069 | 0.1539 | 0.1539 |
Entamoeba histolytica | protein kinase, putative | 0.0039 | 0.0064 | 0.0416 |
Giardia lamblia | Aurora kinase | 0.0069 | 0.1539 | 1 |
Schistosoma mansoni | protein kinase | 0.0065 | 0.1349 | 0.8764 |
Brugia malayi | serine/threonine kinase 12 | 0.0069 | 0.1539 | 0.1539 |
Loa Loa (eye worm) | AUR protein kinase | 0.0069 | 0.1539 | 0.1539 |
Entamoeba histolytica | protein kinase, putative | 0.0039 | 0.0064 | 0.0416 |
Toxoplasma gondii | aurora kinase | 0.0069 | 0.1539 | 0.5 |
Echinococcus multilocularis | aurora kinase A | 0.0069 | 0.1539 | 0.189 |
Entamoeba histolytica | protein kinase, putative | 0.0065 | 0.1349 | 0.8764 |
Entamoeba histolytica | serine/threonine- protein kinase 6, putative | 0.0069 | 0.1539 | 1 |
Trichomonas vaginalis | STE family protein kinase | 0.0065 | 0.1349 | 0.8711 |
Entamoeba histolytica | serine/threonine- protein kinase 6 , putative | 0.0069 | 0.1539 | 1 |
Echinococcus multilocularis | serine:threonine protein kinase 12 B | 0.0069 | 0.1539 | 0.189 |
Entamoeba histolytica | protein kinase domain containing protein | 0.0069 | 0.1539 | 1 |
Entamoeba histolytica | protein kinase , putative | 0.0069 | 0.1539 | 1 |
Entamoeba histolytica | protein kinase, putative | 0.0069 | 0.1539 | 1 |
Schistosoma mansoni | protein kinase | 0.0065 | 0.1349 | 0.8764 |
Echinococcus granulosus | serine:threonine protein kinase PAK 3 | 0.0065 | 0.1349 | 0.1656 |
Brugia malayi | serine/threonine protein kinase 6 | 0.0069 | 0.1539 | 0.1539 |
Echinococcus multilocularis | serine:threonine protein kinase PAK 3 | 0.0065 | 0.1349 | 0.1656 |
Schistosoma mansoni | protein kinase | 0.0039 | 0.0064 | 0.0416 |
Trichomonas vaginalis | AGC family protein kinase | 0.0069 | 0.1539 | 1 |
Echinococcus multilocularis | serine:threonine protein kinase PAK 3 | 0.0065 | 0.1349 | 0.1656 |
Plasmodium vivax | serine/threonine protein kinase 6, putative | 0.0069 | 0.1539 | 0.5 |
Entamoeba histolytica | p21-activated kinase | 0.0065 | 0.1349 | 0.8764 |
Trypanosoma cruzi | aurora B kinase, putative | 0.0069 | 0.1539 | 0.5 |
Trichomonas vaginalis | AGC family protein kinase | 0.0069 | 0.1539 | 1 |
Schistosoma mansoni | protein kinase | 0.0069 | 0.1539 | 1 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0064 | 0.1284 | 0.8276 |
Brugia malayi | serine/threonine-protein kinase 6 | 0.0069 | 0.1539 | 0.1539 |
Entamoeba histolytica | protein kinase, putative | 0.0069 | 0.1539 | 1 |
Echinococcus granulosus | serine:threonine protein kinase 12 B | 0.0069 | 0.1539 | 0.189 |
Echinococcus granulosus | serine:threonine protein kinase PAK 4 | 0.0203 | 0.8142 | 1 |
Echinococcus granulosus | aurora kinase A | 0.0069 | 0.1539 | 0.189 |
Echinococcus multilocularis | serine:threonine protein kinase PAK 4 | 0.0203 | 0.8142 | 1 |
Trichomonas vaginalis | AGC family protein kinase | 0.0069 | 0.1539 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 362 nM | Inhibition of PAK1 in human EBC1 cells assessed as inhibition of MEK phosphorylation at S298 after 2 hrs by HTRF assay | ChEMBL. | 26030457 |
Ki (binding) | = 5 nM | Inhibition of human recombinant PAK1 kinase domain using coumarin/fluorescein-labeled FRET peptide as substrate assessed as substrate phosphorylation at Ser/Thr19 preincubated for 10 mins followed by ATP addition measured after 60 mins by Z'-LYTE assay | ChEMBL. | 26030457 |
Ki (binding) | = 455 nM | Inhibition of human recombinant PAK4 kinase domain using coumarin/fluorescein-labeled FRET peptide as substrate assessed as substrate phosphorylation at Ser/Thr19 preincubated for 10 mins followed by ATP addition measured after 60 mins by Z'-LYTE assay | ChEMBL. | 26030457 |
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.