begacestat [Ligand Id: 6979] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL463981 (Begacestat, GSI-953)
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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 (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta42 secretion by ELISA B 6.38 pIC50 414 nM IC50 J. Med. Chem. (2013) 56: 1443-1454 [PMID:23342950]
ChEMBL Inhibition of gamma secretase (unknown origin) mediated Notch M1726V mutant activation in CHO K1 cells after 48 hrs by chemiluminescence assay B 6.68 pIC50 208.5 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]
ChEMBL Inhibition of gamma-secretase (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta40 secretion by ELISA B 6.69 pIC50 203 nM IC50 J. Med. Chem. (2013) 56: 1443-1454 [PMID:23342950]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2009) 52: 6169-6188 [PMID:19694467]
ChEMBL Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloid beta 40 after 24 hrs by sandwich ELISA B 7.83 pIC50 14.8 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]
ChEMBL Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2013) 56: 5261-5274 [PMID:23713656]
ChEMBL Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA B 7.98 pIC50 10.5 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 996-1000 [PMID:23312944]
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 8.1 pIC50 8 nM IC50 J. Med. Chem. (2009) 52: 6169-6188 [PMID:19694467]
ChEMBL Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA B 8.8 pIC50 1.6 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 996-1000 [PMID:23312944]
ChEMBL Inhibition of partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein measured after overnight incubation by ELISA B 8.8 pIC50 1.6 nM IC50 J. Med. Chem. (2013) 56: 5261-5274 [PMID:23713656]
GtoPdb - - 7.83 pEC50 14.8 nM EC50 J Pharmacol Exp Ther (2009) 331: 598-608 [PMID:19671883]

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]