Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | choline kinase alpha | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Trypanosoma brucei | choline/ethanolamine kinase | choline kinase alpha | 457 aa | 474 aa | 22.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | metabotropic glutamate receptor | 0.0242 | 0.0052 | 0.0052 |
Loa Loa (eye worm) | hypothetical protein | 1.9682 | 1 | 1 |
Echinococcus granulosus | metabotropic glutamate receptor 5 | 0.0356 | 0.011 | 0.0058 |
Brugia malayi | metabotropic glutamate receptor subtype 5a (mGluR5a), putative | 0.0262 | 0.0062 | 0.0062 |
Brugia malayi | STAT protein, DNA binding domain containing protein | 0.0312 | 0.0088 | 0.0088 |
Echinococcus granulosus | alpha 16 mannosyl glycoprotein | 1.9682 | 1 | 1 |
Schistosoma mansoni | beta-12-n-acetylglucosaminyltransferase II | 1.9682 | 1 | 1 |
Toxoplasma gondii | 1,3-beta-glucan synthase component protein | 0.1296 | 0.0591 | 0.5 |
Echinococcus multilocularis | alpha 1,6 mannosyl glycoprotein | 1.9682 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0356 | 0.011 | 0.0034 |
Brugia malayi | Metabotropic glutamate receptor precursor. | 0.0289 | 0.0076 | 0.0076 |
Schistosoma mansoni | metabotropic glutamate receptor 2 3 (mglur group 2) | 0.0328 | 0.0096 | 0.0096 |
Loa Loa (eye worm) | STAT protein | 0.0312 | 0.0088 | 0.0012 |
Echinococcus multilocularis | metabotropic glutamate receptor 5 | 0.0356 | 0.011 | 0.0058 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (ADMET) | 0 | Cytotoxicity against human erythrocytes assessed as hemolytic activity at 500 uM | ChEMBL. | 17383187 |
EC50 (binding) | = 1.3 uM | Inhibition of CHKA in human HCT116 cells assessed as [3H]phosphocholine formation using [3H]choline chloride as substrate incubated for 1 hr prior to substrate addition measured after 1 hr by scintillation counting analysis | ChEMBL. | 24976941 |
GI50 (functional) | = 0.38 uM | Growth inhibition of human A549 cells overexpressing CHKA2 after 72 hrs by sulforhodamine assay | ChEMBL. | 24976941 |
Inhibition (binding) | = 40 % | Inhibition of phospholipase B activity of PLB1 in Cryptococcus neoformans var. grubii H99 assessed as loss of 1,2-di[1-14C]palmitoyl phosphatidylcholine at 250 uM | ChEMBL. | 17383187 |
Inhibition (binding) | = 40 % | Inhibition of phospholipase B activity of PLB1 in Cryptococcus neoformans var. grubii H99 assessed as loss of 1,2-di[1-14C]palmitoyl phosphatidylcholine at 250 uM | ChEMBL. | 17383187 |
Inhibition (binding) | > 75 % | Inhibition of CHKA in human HCT116 cells assessed as [3H]phosphocholine formation using [3H]choline chloride as substrate at 2.4 +/-1 uM incubated for 1 hr prior to substrate addition measured after 1 hr by scintillation counting analysis | ChEMBL. | 24976941 |
Inhibition (binding) | > 75 % | Inhibition of CHKA in human HCT116 cells assessed as [3H]phosphocholine formation using [3H]choline chloride as substrate at 6.5 +/-4 uM incubated for 1 hr prior to substrate addition measured after 1 hr by scintillation counting analysis | ChEMBL. | 24976941 |
MIC (functional) | = 2.8 uM | Antifungal activity against Cryptococcus neoformans ATCC 90112 | ChEMBL. | 17383187 |
MIC (functional) | = 2.8 uM | Antifungal activity against Candida albicans ATCC 10231 | ChEMBL. | 17383187 |
MIC (functional) | = 2.8 uM | Antifungal activity against Cryptococcus neoformans ATCC 90112 | ChEMBL. | 17383187 |
MIC (functional) | = 2.8 uM | Antifungal activity against Candida albicans ATCC 10231 | ChEMBL. | 17383187 |
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.
2 literature references were collected for this gene.