necrostatin-1s [Ligand Id: 9751] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL381230
  • receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
GtoPdb Affinity constant measured at 37oC. - 7.43 pKd 37 nM Kd Proc Natl Acad Sci USA (1998) 95: 11211-6 [PMID:9736715]
ChEMBL Inhibition of human recombinant RIPK1 after 4 hrs by ADP-Glo assay B 6.12 pIC50 754 nM IC50 J Med Chem (2018) 61: 1895-1920 [PMID:29437386]
ChEMBL Inhibition of RIPK1 (1 to 312 residues) (unknown origin) preincubated for 15 mins followed by addition of [gamma32P] ATP and measured after 30 mins by SDS-PAGE based autoradiography B 6.49 pIC50 320 nM IC50 J Med Chem (2020) 63: 1490-1510 [PMID:31622096]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]