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

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ChEMBL ligand: CHEMBL1090771 (Avagacestat, BMS 708163, BMS-708163, BMS-70816301, BMS-708163-01)
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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: 2402, 2403] [UniProtKB: P49768, P49810, Q8WW43, Q92542, Q96BI3, Q9NZ42]
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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]