Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | tyrosine kinase 2 | Starlite/ChEMBL | References |
Homo sapiens | Janus kinase 3 | Starlite/ChEMBL | References |
Homo sapiens | Janus kinase 1 | Starlite/ChEMBL | References |
Homo sapiens | Janus kinase 2 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | SRC-1 | 0.0015 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase lyn lyn a protein tyrosine kinase lymphocyte specific protein tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.0015 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0015 | 0.5 | 0.5 | |
Echinococcus multilocularis | tyrosine protein kinase Fps85D | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src64B | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine kinase|tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Brugia malayi | Tyrosine-protein kinase abl-1 | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase lyn tyrosine protein kinase blk | 0.0015 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0015 | 0.5 | 0.5 | |
Echinococcus granulosus | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Src64B | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Entamoeba histolytica | SH2-protein kinase domain containing protein | 0.0015 | 0.5 | 0.5 |
Schistosoma mansoni | proto-oncogene tyrosine-protein kinase src | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Abl | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Blk | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase shark | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase ABL1 | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | c src tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase ABL1 | 0.0015 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.0015 | 0.5 | 0.5 |
Brugia malayi | protein-tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0015 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fps85D | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fgr | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Btk29A | 0.0015 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0015 | 0.5 | 0.5 | |
Echinococcus multilocularis | tyrosine protein kinase Blk | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Srms | 0.0015 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0015 | 0.5 | 0.5 | |
Echinococcus granulosus | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK protein kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | c src tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | proto oncogene tyrosine protein kinase LCK | 0.0015 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0015 | 0.5 | 0.5 | |
Echinococcus granulosus | tyrosine protein kinase shark | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0015 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0015 | 0.5 | 0.5 | |
Echinococcus multilocularis | tyrosine protein kinase Btk29A | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | 3'partial|tyrosine protein kinase Fgr | 0.0015 | 0.5 | 0.5 |
Brugia malayi | hypothetical protein | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Lyn | 0.0015 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Src42A | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | proto oncogene tyrosine protein kinase LCK | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | SRC-1 | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src42A | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/ABL protein kinase | 0.0015 | 0.5 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0015 | 0.5 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0015 | 0.5 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Srms | 0.0015 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Fu (ADMET) | = 1.2 % | Fraction unbound in human plasma by equilibrium dialysis | ChEMBL. | 22087750 |
IC50 (binding) | = 0.001 uM | Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay | ChEMBL. | 22087750 |
IC50 (binding) | = 0.03 uM | Inhibition of human recombinant N-terminal GST-tagged JAK1 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay | ChEMBL. | 22087750 |
IC50 (binding) | = 0.048 uM | Inhibition of JAK2 in human PBMC assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining | ChEMBL. | 22087750 |
IC50 (binding) | = 0.266 uM | Inhibition of human recombinant N-terminal GST-tagged TYK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay | ChEMBL. | 22087750 |
IC50 (binding) | = 0.307 uM | Inhibition of human recombinant N-terminal GST-tagged JAK3 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay | ChEMBL. | 22087750 |
IC50 (binding) | = 0.625 uM | Inhibition of JAK1/JAK3 in human PBMC assessed as inhibition of IL2-stimulated STATs phosphorylation preincubated for 30 mins prior to IL2 challenge measured after 15 mins by intracellular phosflow staining | ChEMBL. | 22087750 |
IC50 (binding) | = 1.01 uM | Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay | ChEMBL. | 22087750 |
IC50 (binding) | = 1.09 uM | Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay | ChEMBL. | 22087750 |
IC50 (binding) | = 1.48 uM | Inhibition of JAK2 in human whole blood assessed as inhibition of TPO-stimulated STAT5 phosphorylation preincubated for 30 mins prior to TPO challenge measured after 15 mins by intracellular phosflow staining | ChEMBL. | 22087750 |
IC50 (binding) | > 25 uM | Inhibition of TEL-fused JAK3 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay | ChEMBL. | 22087750 |
IC50 (binding) | > 25 uM | Inhibition of TEL-fused TYK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay | ChEMBL. | 22087750 |
IC50 (binding) | > 25 uM | Inhibition of JAK1/JAK3 in human whole blood assessed as inhibition of IL2-stimulated STATs phosphorylation preincubated for 30 mins prior to IL2 challenge measured after 15 mins by intracellular phosflow staining | ChEMBL. | 22087750 |
Ratio IC50 (binding) | = 37.5 | Ratio of IC50 for JAK2 in human whole blood to IC50 for JAK2 in human PBMC | ChEMBL. | 22087750 |
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.
1 literature reference was collected for this gene.