Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | aurora kinase B | References | |
Homo sapiens | TTK protein kinase | Starlite/ChEMBL | References |
Homo sapiens | inner centromere protein antigens 135/155kDa | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Trypanosoma brucei | mitogen-activated protein kinase 5 | aurora kinase B | 303 aa | 299 aa | 22.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Protein kinase domain containing protein | 0.0088 | 0.0606 | 0.0606 |
Trypanosoma brucei | aurora B kinase | 0.0069 | 0 | 0.5 |
Schistosoma mansoni | dual specificity serine/threonine tyrosine kinase | 0.0088 | 0.0606 | 1 |
Entamoeba histolytica | serine/threonine protein kinase 6, putative | 0.0069 | 0 | 0.5 |
Leishmania major | protein kinase, putative | 0.0069 | 0 | 0.5 |
Entamoeba histolytica | protein kinase, putative | 0.0069 | 0 | 0.5 |
Giardia lamblia | Kinase, TTK | 0.0088 | 0.0606 | 1 |
Entamoeba histolytica | serine/threonine- protein kinase 6 , putative | 0.0069 | 0 | 0.5 |
Echinococcus granulosus | dual specificity serine:threonine tyrosine | 0.0088 | 0.0606 | 1 |
Entamoeba histolytica | protein kinase, putative | 0.0069 | 0 | 0.5 |
Entamoeba histolytica | protein kinase domain containing protein | 0.0069 | 0 | 0.5 |
Entamoeba histolytica | protein kinase , putative | 0.0069 | 0 | 0.5 |
Toxoplasma gondii | aurora kinase | 0.0069 | 0 | 0.5 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0088 | 0.0606 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0382 | 1 | 1 |
Echinococcus multilocularis | dual specificity serine:threonine tyrosine | 0.0088 | 0.0606 | 1 |
Plasmodium falciparum | serine/threonine protein kinase, putative | 0.0069 | 0 | 0.5 |
Plasmodium vivax | serine/threonine protein kinase 6, putative | 0.0069 | 0 | 0.5 |
Loa Loa (eye worm) | TTK protein kinase | 0.0088 | 0.0606 | 0.0606 |
Entamoeba histolytica | serine/threonine- protein kinase 6, putative | 0.0069 | 0 | 0.5 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0088 | 0.0606 | 1 |
Trypanosoma cruzi | aurora B kinase, putative | 0.0069 | 0 | 0.5 |
Onchocerca volvulus | Dual specificity protein kinase TTK homolog | 0.0088 | 0.0606 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
GI50 (functional) | = 0.021 uM | Cytotoxicity against human MDA-MB-468 cells after 5 days by sulforhodamine B assay | ChEMBL. | 25763473 |
IC50 (ADMET) | Inhibition of human CYP3A4 using BFC as substrate preincubated for 10 mins followed by enzyme/substrate addition measured after 30 mins by fluorescence assay | ChEMBL. | 25763473 | |
IC50 (binding) | = 0.006 uM | Inhibition of amino terminal GST-fused full length human TTK using His6-SUMO-TTK-N as substrate preincubated for 15 mins prior to ATP addition by indirect ELISA detection system | ChEMBL. | 25763473 |
IC50 (binding) | > 6.3 uM | Inhibition of AURKB/INCENP (unknown origin) preincubated for 15 mins prior to ATP addition by FRET-based homogenous assay | ChEMBL. | 25763473 |
T1/2 (ADMET) | = 34 min | Half life in mouse liver microsomes at 1 uM by LC-MS analysis | ChEMBL. | 25763473 |
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.