Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | Janus kinase 1 | No references | |
Homo sapiens | Janus kinase 2 | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | tyrosine protein kinase Fps85D | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | proto-oncogene tyrosine-protein kinase src | 0.001 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src64B | 0.001 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine kinase|tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Echinococcus multilocularis | proto oncogene tyrosine protein kinase LCK | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase lyn lyn a protein tyrosine kinase lymphocyte specific protein tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | c src tyrosine kinase | 0.001 | 0.5 | 0.5 |
Brugia malayi | SRC-1 | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/ABL protein kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Blk | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | 3'partial|tyrosine protein kinase Fgr | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fps85D | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Abl | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Src64B | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Blk | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Btk29A | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | SRC-1 | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase ABL1 | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase shark | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | proto oncogene tyrosine protein kinase LCK | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Srms | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase shark | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | c src tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Srms | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase lyn tyrosine protein kinase blk | 0.001 | 0.5 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.001 | 0.5 | 0.5 |
Entamoeba histolytica | SH2-protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Lyn | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase ABL1 | 0.001 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Btk29A | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK protein kinase | 0.001 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Brugia malayi | protein-tyrosine kinase | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Brugia malayi | SH2 domain containing protein | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Src42A | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src42A | 0.001 | 0.5 | 0.5 |
Brugia malayi | hypothetical protein | 0.001 | 0.5 | 0.5 |
Brugia malayi | Tyrosine-protein kinase abl-1 | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fgr | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 2 nM | HTRF Assay | BINDINGDB. | No reference |
IC50 (binding) | = 26 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.