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 granulosus | tyrosine protein kinase ABL1 | 0.001 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK protein kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Btk29A | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 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 |
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 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fgr | 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 Src42A | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src42A | 0.001 | 0.5 | 0.5 |
Brugia malayi | SH2 domain containing protein | 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 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Schistosoma mansoni | tyrosine kinase | 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 |
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 granulosus | tyrosine protein kinase Btk29A | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase ABL1 | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | SRC-1 | 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 shark | 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 | c src tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Srms | 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 | |
Entamoeba histolytica | SH2-protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Lyn | 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 |
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 |
Brugia malayi | SRC-1 | 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 |
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 |
Echinococcus granulosus | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Abl | 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 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 |
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 Fps85D | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 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 |
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 multilocularis | proto oncogene tyrosine protein kinase LCK | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | c src tyrosine kinase | 0.001 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 4 nM | HTRF Assay | BINDINGDB. | No reference |
IC50 (binding) | = 33 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.