Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | Janus kinase 2 | Starlite/ChEMBL | No references |
Homo sapiens | Janus kinase 1 | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Pre-SET motif family protein | 0.0241 | 0.8739 | 0.8851 |
Schistosoma mansoni | alpha-galactosidase/alpha-n-acetylgalactosaminidase | 0.0017 | 0.0245 | 0.0597 |
Loa Loa (eye worm) | follicle stimulating hormone receptor | 0.0271 | 0.9873 | 1 |
Echinococcus multilocularis | histone lysine methyltransferase setb histone lysine methyltransferase eggless | 0.0035 | 0.0918 | 0.2239 |
Schistosoma mansoni | histone-lysine n-methyltransferase setb1 | 0.0035 | 0.0918 | 0.2239 |
Schistosoma mansoni | histone-lysine n-methyltransferase suv9 | 0.0035 | 0.0918 | 0.2239 |
Onchocerca volvulus | 0.0035 | 0.0918 | 0.0918 | |
Echinococcus multilocularis | Alpha N acetylgalactosaminidase | 0.0118 | 0.4102 | 1 |
Echinococcus multilocularis | Glycoside hydrolase, family 27 | 0.0118 | 0.4102 | 1 |
Brugia malayi | follicle stimulating hormone receptor | 0.0271 | 0.9873 | 1 |
Echinococcus multilocularis | tyrosine protein kinase shark | 0.001 | 0.000000054851 | 0.00000013372 |
Brugia malayi | Melibiase family protein | 0.0079 | 0.2605 | 0.2639 |
Schistosoma mansoni | alpha-galactosidase/alpha-n-acetylgalactosaminidase | 0.0118 | 0.4102 | 1 |
Echinococcus multilocularis | histone lysine N methyltransferase SETMAR | 0.0035 | 0.0918 | 0.2239 |
Entamoeba histolytica | SH2-protein kinase domain containing protein | 0.001 | 0 | 0.5 |
Schistosoma mansoni | alpha-galactosidase/alpha-n-acetylgalactosaminidase | 0.0079 | 0.2605 | 0.6351 |
Plasmodium vivax | SET domain protein, putative | 0.0035 | 0.0918 | 0.5 |
Brugia malayi | Pre-SET motif family protein | 0.0035 | 0.0918 | 0.093 |
Loa Loa (eye worm) | pre-SET domain-containing protein family protein | 0.0241 | 0.8739 | 0.8851 |
Loa Loa (eye worm) | hypothetical protein | 0.0079 | 0.2605 | 0.2639 |
Schistosoma mansoni | alpha-galactosidase/alpha-n-acetylgalactosaminidase | 0.0118 | 0.4102 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0035 | 0.0918 | 0.093 |
Echinococcus granulosus | histone lysine methyltransferase setb | 0.0035 | 0.0918 | 0.2239 |
Toxoplasma gondii | histone lysine methyltransferase SET/SUV39 | 0.0035 | 0.0918 | 0.1746 |
Trichomonas vaginalis | set domain proteins, putative | 0.0274 | 1 | 1 |
Schistosoma mansoni | alpha-galactosidase/alpha-n-acetylgalactosaminidase | 0.0118 | 0.4102 | 1 |
Echinococcus granulosus | 5'partial|histone lysine N methyltransferase SETDB2 | 0.0033 | 0.087 | 0.2121 |
Toxoplasma gondii | melibiase subfamily protein | 0.0118 | 0.4102 | 1 |
Schistosoma mansoni | hypothetical protein | 0.006 | 0.1878 | 0.4577 |
Schistosoma mansoni | alpha-galactosidase/alpha-n-acetylgalactosaminidase | 0.0079 | 0.2605 | 0.6351 |
Schistosoma mansoni | histone-lysine n-methyltransferase setb1 | 0.0035 | 0.0918 | 0.2239 |
Echinococcus granulosus | Alpha N acetylgalactosaminidase | 0.0118 | 0.4102 | 1 |
Schistosoma mansoni | histone-lysine n-methyltransferase setb1 | 0.0035 | 0.0918 | 0.2239 |
Schistosoma mansoni | alpha-galactosidase/alpha-n-acetylgalactosaminidase | 0.0118 | 0.4102 | 1 |
Echinococcus granulosus | tyrosine protein kinase shark | 0.001 | 0.000000054851 | 0.00000013372 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.000000054851 | 0.00000013372 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 10 nM | BindingDB_Patents: HTRF Assay. The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction. | ChEMBL. | No reference |
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.