avagacestat [Ligand Id: 6489] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1090771 (BMS-708163, Avagacestat, BMS 708163, BMS-708163-01, BMS-70816301)
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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 IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA B 8.82 pIC50 1.5 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 996-1000 [PMID:23312944]
ChEMBL Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2013) 56: 5261-5274 [PMID:23713656]
GtoPdb - - 9.5 pIC50 0.3 nM IC50 DRUGS IN CLINICAL TRIALS: BMS-708163.. Alzheimer Research Forum
ChEMBL Inhibition of human gamma secretase-mediated amyloid beta (1 to 40) production expressed in human H4 cells B 9.52 pIC50 0.3 nM IC50 J. Med. Chem. (2009) 52: 6169-6188 [PMID:19694467]
ChEMBL Inhibition of gamma-secretase in human H4-8Sw cells assessed as reduction in amyloid beta (1 to 42) formation B 9.57 pIC50 0.27 nM IC50 Eur J Med Chem (2018) 148: 436-452 [PMID:29477076]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta42 production in human H4 cells expressing human APP swedish mutant B 9.65 pIC50 0.23 nM IC50 J. Med. Chem. (2012) 55: 3414-3424 [PMID:22420884]
ChEMBL Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA B 9.89 pIC50 0.13 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 9.89 pIC50 0.13 nM IC50 J. Med. Chem. (2013) 56: 5261-5274 [PMID:23713656]

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]