Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | Janus kinase 2 | Starlite/ChEMBL | No references |
Homo sapiens | Janus kinase 3 | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Schistosoma mansoni | proto-oncogene tyrosine-protein kinase src | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase ABL1 | 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 Src42A | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Srms | 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 |
Brugia malayi | Protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 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 Src64B | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/ABL 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 | |
Echinococcus granulosus | c src tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Blk | 0.001 | 0.5 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fps85D | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | c src tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Srms | 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 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | 3'partial|tyrosine protein kinase Fgr | 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 | |
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 granulosus | tyrosine protein kinase Fyn | 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 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 shark | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fps85D | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fgr | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase lyn tyrosine protein kinase blk | 0.001 | 0.5 | 0.5 |
Onchocerca volvulus | 0.001 | 0.5 | 0.5 | |
Loa Loa (eye worm) | TK protein kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Lyn | 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 Btk29A | 0.001 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.001 | 0.5 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 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 |
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 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | proto oncogene tyrosine protein kinase LCK | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Blk | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Abl | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | SRC-1 | 0.001 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.001 | 0.5 | 0.5 |
Brugia malayi | hypothetical protein | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src64B | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Src42A | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase ABL1 | 0.001 | 0.5 | 0.5 |
Brugia malayi | SRC-1 | 0.001 | 0.5 | 0.5 |
Brugia malayi | protein-tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Btk29A | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase shark | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine kinase|tyrosine protein kinase Fyn | 0.001 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.001 | 0.5 | 0.5 |
Echinococcus granulosus | proto oncogene tyrosine protein kinase LCK | 0.001 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.033 nM | HTRF Assay | BINDINGDB. | No reference |
IC50 (binding) | > 1496 nM | BindingDB_Patents: HTRF Assay. The ability of compounds to inhibit the activity of JAKl, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAKl #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 nL 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 of 1.1 IX enzyme and 1.1 IX substrate in IX 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 room temperature to allow compound binding to equilibrate. After equilibration, 2 \xL of 10X ATP in IX assay buffer was added to initiate the kinase reaction and the plates were shaken. | 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.