SCH-900229 [Ligand Id: 8848] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2159511 (SCH-900229)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
presenilin 1/presenilin 2/Gamma-secretase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094135] [GtoPdb: 24022403] [UniProtKB: P49768P49810Q8WW43Q92542Q96BI3Q9NZ42]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 844-849 [PMID:23265892]
ChEMBL Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 850-853 [PMID:23265902]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cell membranes transfected with human APPSOW and APPLON mutant after 5 hrs by sandwich immunoassay B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 844-849 [PMID:23265892]
ChEMBL Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cell membrane co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 850-853 [PMID:23265902]
GtoPdb Data range indicates inhibition of Aβ42 or Aβ40 production. - 9 pIC50 1 nM IC50 ACS Med Chem Lett (2012) 3: 892-6 [PMID:24900404]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 844-849 [PMID:23265892]
ChEMBL Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-42 production B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 850-853 [PMID:23265902]
presenilin 1/Presenilin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2473] [GtoPdb: 2402] [UniProtKB: P49768]
ChEMBL Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as notch cleavage B 7.34 pIC50 46 nM IC50 ACS Med. Chem. Lett. (2012) 3: 892-896 [PMID:24900404]
ChEMBL Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-40 production B 8.4 pIC50 4 nM IC50 ACS Med. Chem. Lett. (2012) 3: 892-896 [PMID:24900404]
ChEMBL Inhibition of PS1 gamma-secretase assessed as reduction of amyloid beta-40 production by membrane based assay B 8.89 pIC50 1.3 nM IC50 ACS Med. Chem. Lett. (2012) 3: 892-896 [PMID:24900404]
GtoPdb Data range indicates inhibition of Aβ42 or Aβ40 production. - 9 pIC50 1 nM IC50 ACS Med Chem Lett (2012) 3: 892-6 [PMID:24900404]
presenilin 2/Presenilin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3708] [GtoPdb: 2403] [UniProtKB: P49810]
ChEMBL Inhibition of PS2 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-42 production B 9 pIC50 1 nM IC50 ACS Med. Chem. Lett. (2012) 3: 892-896 [PMID:24900404]

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]