compound 34 [PMID: 24749861] [Ligand Id: 8129] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3265274
  • endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460]
ChEMBL Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay B 7.33 pIC50 47 nM IC50 J. Med. Chem. (2014) 57: 4289-4301 [PMID:24749861]
GtoPdb Inhibition of RNAse activity. - 7.33 pIC50 47 nM IC50 J. Med. Chem. (2014) 57: 4289-301 [PMID:24749861]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]