Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | receptor (TNFRSF)-interacting serine-threonine kinase 1 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trypanosoma cruzi | cytochrome P450, putative | 0.0026 | 0.9626 | 0.5 |
Schistosoma mansoni | netrin receptor unc5 | 0.0026 | 1 | 0.5 |
Loa Loa (eye worm) | immunoglobulin I-set domain-containing protein | 0.0026 | 1 | 1 |
Echinococcus granulosus | netrin receptor unc 5 | 0.0026 | 1 | 0.5 |
Echinococcus multilocularis | ankyrin repeat and death domain containing protein | 0.0026 | 1 | 0.5 |
Echinococcus granulosus | death domain containing protein | 0.0026 | 1 | 0.5 |
Schistosoma mansoni | ankyrin 23/unc44 | 0.0026 | 1 | 0.5 |
Loa Loa (eye worm) | CYP4Cod1 | 0.0026 | 0.9626 | 0.9626 |
Trypanosoma brucei | cytochrome P450, putative | 0.0026 | 0.9626 | 0.5 |
Brugia malayi | Protein kinase domain containing protein | 0.0026 | 1 | 1 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0026 | 0.9626 | 0.9626 |
Brugia malayi | Death domain containing protein | 0.0026 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 1 | 1 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0026 | 0.9626 | 0.9626 |
Brugia malayi | Immunoglobulin I-set domain containing protein | 0.0026 | 1 | 1 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0026 | 0.9626 | 0.5 |
Echinococcus multilocularis | netrin receptor unc 5 | 0.0026 | 1 | 0.5 |
Echinococcus granulosus | ankyrin repeat and death domain containing protein | 0.0026 | 1 | 0.5 |
Onchocerca volvulus | Netrin receptor homolog | 0.0026 | 1 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0026 | 1 | 0.5 |
Schistosoma mansoni | retinoblastoma-binding protein 4 (rbbp4) | 0.0026 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 1 | 1 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0026 | 0.9626 | 0.5 |
Leishmania major | cytochrome p450-like protein | 0.0026 | 0.9626 | 0.5 |
Echinococcus granulosus | Ankyrin | 0.0026 | 1 | 0.5 |
Echinococcus multilocularis | Ankyrin | 0.0026 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.063 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) | = 0.13 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) | = 5 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.