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 | |
Homo sapiens | p21 protein (Cdc42/Rac)-activated kinase 3 | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trypanosoma cruzi | p21-activated kinase 3, putative | 0.0079 | 0.2768 | 0.5 |
Echinococcus granulosus | serine:threonine protein kinase PAK 3 | 0.0136 | 1 | 1 |
Echinococcus granulosus | serine:threonine protein kinase PAK 3 | 0.0136 | 1 | 1 |
Loa Loa (eye worm) | STE/STE20/PAKA protein kinase | 0.0079 | 0.2768 | 0.2808 |
Trichomonas vaginalis | mitogen-activated protein kinase kinase kinase 3, MAPKKK3, MEKK3, putative | 0.0079 | 0.2768 | 0.2768 |
Loa Loa (eye worm) | hypothetical protein | 0.0135 | 0.9857 | 1 |
Echinococcus multilocularis | serine:threonine protein kinase PAK 3 | 0.0136 | 1 | 1 |
Schistosoma mansoni | protein kinase | 0.0136 | 1 | 1 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0079 | 0.2768 | 0.2768 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0135 | 0.9857 | 0.9857 |
Entamoeba histolytica | protein kinase, putative | 0.0136 | 1 | 1 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0079 | 0.2768 | 0.2768 |
Trichomonas vaginalis | STE family protein kinase | 0.0136 | 1 | 1 |
Trypanosoma cruzi | STE/STE20 serine/threonine-protein kinase, putative | 0.0079 | 0.2768 | 0.5 |
Loa Loa (eye worm) | STE/STE20/PAKA protein kinase | 0.0079 | 0.2768 | 0.2808 |
Giardia lamblia | Kinase, STE STE20 | 0.0136 | 1 | 0.5 |
Echinococcus granulosus | p21 activated protein kinase 1 Dpak1 | 0.0136 | 1 | 1 |
Echinococcus multilocularis | p21 activated protein kinase 1 Dpak1 | 0.0136 | 1 | 1 |
Trichomonas vaginalis | STE family protein kinase | 0.0136 | 1 | 1 |
Trichomonas vaginalis | STE family protein kinase | 0.0136 | 1 | 1 |
Echinococcus multilocularis | serine:threonine protein kinase PAK 3 | 0.0136 | 1 | 1 |
Schistosoma mansoni | protein kinase | 0.0136 | 1 | 1 |
Brugia malayi | p21/Cdc42/Rac1-activated kinase | 0.0079 | 0.2768 | 0.2768 |
Trichomonas vaginalis | STE family protein kinase | 0.0136 | 1 | 1 |
Entamoeba histolytica | p21-activated kinase | 0.0136 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CL (ADMET) | = 48 ml/min.kg | Plasma clearance in nude mouse at 2 mg/kg, iv | ChEMBL. | 27346791 |
CL (ADMET) | = 1067 ml/min.kg | Unbound clearance in nude mouse at 2 mg/kg, iv | ChEMBL. | 27346791 |
Cmax (ADMET) | = 4.7 uM | Cmax in nude mouse at 25 mg/kg, po | ChEMBL. | 27346791 |
F (ADMET) | = 4.8 % | Oral bioavailability in nude mouse at 25 mg/kg | ChEMBL. | 27346791 |
IC50 (binding) | = 51 nM | Inhibition of PAK1/2/3 in human EBC1 cells assessed as MEK1 phosphorylation level at Serine298 residue incubated for 2 hrs by HTRF assay | ChEMBL. | 27346791 |
Ki (binding) | = 32 nM | Inhibition of recombinant human GST-tagged PAK1 kinase domain expressed in baculovirus expression system assessed as suppression of phosphorylation of coumarin/fluorescein-labelled FRET peptide substrate at Ser/Thr19 residues preincubated with substrate for 10 mins followed by enzyme addition measured after 60 mins by Z-Lyte assay | ChEMBL. | 27346791 |
T1/2 (ADMET) | = 0.63 hr | Half life in nude mouse at 2 mg/kg, iv | ChEMBL. | 27346791 |
Tmax (ADMET) | = 0.58 hr | Tmax in nude mouse at 25 mg/kg, po | ChEMBL. | 27346791 |
Vdss (ADMET) | = 1.65 L/Kg | Volume of distribution at steady state in nude mouse at 2 mg/kg, iv | ChEMBL. | 27346791 |
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.