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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]