Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | neurotrophic tyrosine kinase, receptor, type 1 | Starlite/ChEMBL | No references |
Homo sapiens | Janus kinase 3 | Starlite/ChEMBL | No references |
Homo sapiens | Janus kinase 1 | Starlite/ChEMBL | No references |
Homo sapiens | tyrosine kinase 2 | Starlite/ChEMBL | No references |
Homo sapiens | Janus kinase 2 | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | tyrosine protein kinase lyn lyn a protein tyrosine kinase lymphocyte specific protein tyrosine kinase | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0017 | 1 | 0.5 |
Brugia malayi | SRC-1 | 0.0017 | 1 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0017 | 1 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.0017 | 1 | 0.5 |
Onchocerca volvulus | 0.0017 | 1 | 0.5 | |
Brugia malayi | Protein kinase domain containing protein | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Src64B | 0.0017 | 1 | 0.5 |
Onchocerca volvulus | 0.0017 | 1 | 0.5 | |
Echinococcus granulosus | tyrosine kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase lyn tyrosine protein kinase blk | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src64B | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fps85D | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine kinase|tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Brugia malayi | Tyrosine-protein kinase abl-1 | 0.0017 | 1 | 0.5 |
Entamoeba histolytica | SH2-protein kinase domain containing protein | 0.0017 | 1 | 1 |
Echinococcus multilocularis | tyrosine protein kinase Abl | 0.0017 | 1 | 0.5 |
Schistosoma mansoni | proto-oncogene tyrosine-protein kinase src | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase shark | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Blk | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0017 | 1 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase ABL1 | 0.0017 | 1 | 0.5 |
Brugia malayi | SH2 domain containing protein | 0.0017 | 1 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase ABL1 | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | c src tyrosine kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fgr | 0.0017 | 1 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Fps85D | 0.0017 | 1 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Brugia malayi | protein-tyrosine kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Blk | 0.0017 | 1 | 0.5 |
Onchocerca volvulus | 0.0017 | 1 | 0.5 | |
Echinococcus granulosus | tyrosine protein kinase Btk29A | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | proto oncogene tyrosine protein kinase LCK | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | c src tyrosine kinase | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine kinase | 0.0017 | 1 | 0.5 |
Onchocerca volvulus | 0.0017 | 1 | 0.5 | |
Echinococcus multilocularis | tyrosine protein kinase Srms | 0.0017 | 1 | 0.5 |
Schistosoma mansoni | tyrosine kinase | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Onchocerca volvulus | 0.0017 | 1 | 0.5 | |
Echinococcus multilocularis | tyrosine kinase | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase shark | 0.0017 | 1 | 0.5 |
Onchocerca volvulus | 0.0017 | 1 | 0.5 | |
Echinococcus multilocularis | tyrosine protein kinase Btk29A | 0.0017 | 1 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Lyn | 0.0017 | 1 | 0.5 |
Brugia malayi | hypothetical protein | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | 3'partial|tyrosine protein kinase Fgr | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | proto oncogene tyrosine protein kinase LCK | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Src42A | 0.0017 | 1 | 0.5 |
Echinococcus granulosus | tyrosine protein kinase Srms | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/ABL protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Src42A | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | TK/FER protein kinase | 0.0017 | 1 | 0.5 |
Echinococcus multilocularis | tyrosine protein kinase Fyn | 0.0017 | 1 | 0.5 |
Loa Loa (eye worm) | SRC-1 | 0.0017 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 1.95 nM | BindingDB_Patents: ELISA Assay. An enzyme-linked immunosorbant assay (ELISA) was used to assess TrkA kinase activity in the presence of inhibitors. Immulon 4HBX 384-well microtiter plates (Thermo part #8755) were coated with a 0.025 mg/mL solution of poly (Glu, Ala, Tyr; 6:3:1; Sigma P3899). Various concentrations of test compound, 2.5 nM TrkA (Invitrogen Corp., histidine-tagged recombinant human TrkA, cytoplasmic domain), and 500 uM ATP were incubated for 25 minutes at ambient temperature in the coated plates while shaking The assay buffer consisted of 25 mM MOPS pH 7.5, 0.005% (v/v) Triton X-100 and 5 mM MgCl2. The reaction mixture was removed from the plate by washing with PBS containing 0.1% (v/v) Tween 20. The phosphorylated reaction product was detected using 0.2 ug/mL of a phosphotyrosine specific monoclonal antibody (clone PY20) conjugated to horseradish peroxidase in conjunction with the TMB Peroxidase Substrate System (KPL). | ChEMBL. | No reference |
IC50 (binding) | = 1.95 nM | ELISA Assay | BINDINGDB. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 10 µM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 µL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210). | ChEMBL. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Jak1 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 8 µM Omnia Y12 peptide (Catalog # IVGN KPZ3121C; Invitrogen Corporation, Carlsbad, Calif.) and 5 nM Jak1 in a total volume of 20 µL. GST-tagged human Jak1 kinase domain comprising amino acids 866-1154 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4774). | ChEMBL. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Jak3 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 10 µM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 1.5 nM Jak3 in a total volume of 20 µL. GST-tagged human Jak3 kinase domain comprising amino acids 781-1124 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV3855). | ChEMBL. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Tyk2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 8 µM Omnia Y12 peptide (Catalog # IVGN KPZ3121C; Invitrogen Corporation, Carlsbad, Calif.) and 1 nM Tyk2 in a total volume of 20 µL. Human Tyk2 kinase domain, comprising amino acids 886 to 1187 with 10 additional histidine residues (histidine tag) on the carboxy terminus, was expressed and purified from bacculovirus in-house at Array BioPharma Inc. (Boulder, Colo.). The histidine tag was cleaved after purification using standard conditions. | ChEMBL. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Jak1 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 8 µM Omnia Y12 peptide (Catalog # IVGN KPZ3121C; Invitrogen Corporation, Carlsbad, Calif.) and 5 nM Jak1 in a total volume of 20 µL. GST-tagged human Jak1 kinase domain comprising amino acids 866-1154 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4774). | ChEMBL. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Tyk2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 8 µM Omnia Y12 peptide (Catalog # IVGN KPZ3121C; Invitrogen Corporation, Carlsbad, Calif.) and 1 nM Tyk2 in a total volume of 20 µL. Human Tyk2 kinase domain, comprising amino acids 886 to 1187 with 10 additional histidine residues (histidine tag) on the carboxy terminus, was expressed and purified from bacculovirus in-house at Array BioPharma Inc. (Boulder, Colo.). The histidine tag was cleaved after purification using standard conditions. | ChEMBL. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Jak2 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 10 µM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 4 nM Jak2 in a total volume of 20 µL. Human Jak2 kinase domain comprising amino acids 808-1132 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV4210). | ChEMBL. | No reference |
IC50 (binding) | > 1000 nM | BindingDB_Patents: Inhibition Assay. Compounds of Formula I were screened for their ability to inhibit Jak3 using the general enzyme inhibition assay method, in which the assay mixture contained 500 µM ATP, 10 µM Omnia Y7 peptide (Catalog # IVGN KNZ3071C, Invitrogen Corporation, Carlsbad, Calif.) and 1.5 nM Jak3 in a total volume of 20 µL. GST-tagged human Jak3 kinase domain comprising amino acids 781-1124 was purchased from Invitrogen Corporation, Carlsbad, Calif. (catalog # IVGN PV3855). | 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.