Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | receptor (TNFRSF)-interacting serine-threonine kinase 1 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | death domain containing protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | netrin receptor unc5 | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | ankyrin repeat and death domain containing protein | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Immunoglobulin I-set domain containing protein | 0.0026 | 0.5 | 0.5 |
Onchocerca volvulus | Netrin receptor homolog | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | netrin receptor unc 5 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | ankyrin repeat and death domain containing protein | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | Ankyrin | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Death domain containing protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | ankyrin 23/unc44 | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | Ankyrin | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | immunoglobulin I-set domain-containing protein | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | retinoblastoma-binding protein 4 (rbbp4) | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | netrin receptor unc 5 | 0.0026 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.16 uM | Displacement of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2'',3'']indolizino[8'',7'':5',6']pyrano[3',2':3,4]pyrido[1,2-a]indol-5-ium-2-sulfonate from human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells preincubated for 10 mins followed by fluorescent ligand addition measured after 15 mins by fluorescence polarization assay | ChEMBL. | 24900635 |
IC50 (binding) | = 0.5 uM | Inhibition of human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) autophosphorylation expressed in baculovirus infected insect Sf9 cells after 4 hrs by ADP-Glo luminescence assay | ChEMBL. | 24900635 |
IC50 (binding) | = 1.3 uM | Inhibition of RIP1 in human U937 cells assessed as prevention of TNFalpha/zVAD.fmk-induced necrotic cell death preincubated for 30 to 60 mins followed by TNF-alpha induction measured after overnight incubation by Cell Titer-Glo luminescence assay | ChEMBL. | 24900635 |
Ratio IC50 (binding) | = 10 | Ratio of IC50 for RIP1 in TNFalpha/zVAD.fmk-stimulated human U937 cells by Cell Titer-Glo luminescence assay to IC50 for human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells by fluorescence polarization assay | ChEMBL. | 24900635 |
Ratio IC50 (binding) | = 10 | Ratio of IC50 for RIP1 in TNFalpha/zVAD.fmk-stimulated human U937 cells by Cell Titer-Glo luminescence assay to IC50 for human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescence assay | ChEMBL. | 24900635 |
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.