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ChEMBL ligand: CHEMBL4452233 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] | ||||||||
ChEMBL | Binding affinity to RIP1 (unknown origin) by fluorescence polarization assay | B | 7.7 | pIC50 | 19.95 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1160-1161 [PMID:30613318] |
GtoPdb | Inhibition of enzyme activity of recombinant human RIPK1 (aa 1 to 375) | - | 8.2 | pIC50 | 6.3 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL | Inhibition of RIP1 in human U937 cells assessed as reduction in necroptosis incubated for 24 hrs by cell titer-glo luminescent cell viability assay | B | 8.2 | pIC50 | 6.3 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL | Inhibition of pDEST8HisGSTTev-tagged human RIP1 (1 to 375 residues) expressed in baculovirus infected insect cells preincubated with enzyme for 1 hr followed by ATP addition and measured after 5 hrs by ADP-Glo kinase assay | B | 8.2 | pIC50 | 6.3 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL | Inhibition of RIP1 in human whole blood assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated MIP-1 beta cytokine overproduction incubated for 6 hrs by sandwich ELISA | B | 8.3 | pIC50 | 5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL | Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated necroptosis by measuring cellular ATP levels measured at 21 hrs post stimulation by cell-Titer Glo luminescent cell viability assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
GtoPdb | Cellular activity: inhibition of TNFα-induced necroptosis of human neutrophils | - | 9.3 | pIC50 | 0.5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL | Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated necroptosis by measuring LDH release measured at 21 hrs post stimulation by LDH assay | B | 9.3 | pIC50 | 0.5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL | Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated MIP-1 beta cytokine overproduction measured at 21 hrs post stimulation by sandwich ELISA | B | 9.4 | pIC50 | 0.4 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL | Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated MIP-1 beta mRNA overexpression measured at 21 hrs post-stimulation | B | 9.4 | pIC50 | 0.4 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784911] [GtoPdb: 2189] [UniProtKB: Q60855] | ||||||||
ChEMBL | Inhibition of RIP1 in mouse L929 cells assessed as reduction in necroptosis incubated for 24 hrs by cell titer-glo luminescent cell viability assay | B | 5.89 | pIC50 | 1300 | nM | IC50 | ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]