semagacestat [Ligand Id: 6978] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL520733 (LY450139, LY-450139, Semagacestat)
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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 in human SHSY5Y cells expressing human recombinant APP assessed as effect on Abeta40 level after 24 hrs by DELFIA B 6.7 pIC50 199.53 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1306-1311 [PMID:20056541]
ChEMBL Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as decrease in Abeta42 level after 24 hrs by DELFIA B 6.9 pIC50 125.89 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1306-1311 [PMID:20056541]
ChEMBL Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as decrease in total Abeta level after 24 hrs by DELFIA B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1306-1311 [PMID:20056541]
ChEMBL Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as amyloid beta40 formation by ELISA B 7.4 pIC50 39.81 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1306-1311 [PMID:20056541]
ChEMBL Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as amyloid beta42 formation by ELISA B 7.4 pIC50 39.81 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1306-1311 [PMID:20056541]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells B 7.42 pIC50 38 nM IC50 J. Med. Chem. (2009) 52: 6169-6188 [PMID:19694467]
ChEMBL Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay B 7.42 pIC50 38 nM IC50 J. Med. Chem. (2009) 52: 6169-6188 [PMID:19694467]
GtoPdb - - 7.82 pIC50 15 nM IC50 J Med Chem (2009) 52: 6169-88 [PMID:19694467]
ChEMBL Inhibition of gamma secretase (unknown origin) mediated Notch signaling B 7.85 pIC50 14.1 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]
ChEMBL Inhibition of gamma secretase (unknown origin) B 7.96 pIC50 10.9 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]
ChEMBL Inhibition of partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein measured after overnight incubation by ELISA B 8.1 pIC50 7.9 nM IC50 J. Med. Chem. (2013) 56: 5261-5274 [PMID:23713656]
ChEMBL Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA B 8.49 pIC50 3.2 nM IC50 J. Med. Chem. (2013) 56: 5261-5274 [PMID:23713656]
ChEMBL Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as increase in Abeta38 level after 24 hrs by DELFIA B 6.9 pEC50 125.89 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1306-1311 [PMID:20056541]

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]