E2012 [Ligand Id: 7358] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1224151
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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 Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as reduction of total amyloid beta level after 5 hrs by sandwich immunoassay B 4.85 pIC50 14000 nM IC50 J Med Chem (2012) 55: 489-502 [PMID:22098494]
ChEMBL Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta40 production after 5 hrs by sandwich immunoassay B 5.64 pIC50 2300 nM IC50 J Med Chem (2012) 55: 489-502 [PMID:22098494]
ChEMBL Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 40 production after 16 hrs by sandwich ELISA B 6.25 pIC50 560 nM IC50 Bioorg Med Chem Lett (2015) 25: 3495-3500 [PMID:26142947]
ChEMBL Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw assessed as inhibition of amyloid beta-42 production after 16 to 18 hrs by HTRF assay B 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (2013) 23: 6447-6454 [PMID:24139583]
ChEMBL Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA B 7.07 pIC50 85 nM IC50 Bioorg Med Chem Lett (2015) 25: 3495-3500 [PMID:26142947]
ChEMBL Inhibition of gamma-secretase (unknown origin) B 7.08 pIC50 83 nM IC50 Eur J Med Chem (2018) 148: 436-452 [PMID:29477076]
ChEMBL Modulation of gamma-secretase in human SK-N-BE(2) cells expressing wild type APP 695 assessed as reduction in amyloid beta 42 level after overnight incubation by sandwich immunoassay B 7.09 pIC50 81 nM IC50 J Med Chem (2012) 55: 9089-9106 [PMID:22650177]
ChEMBL Modulation of gamma-secretase (unknown origin) assessed as reduction in amyloid beta 42 level B 7.1 pIC50 80 nM IC50 ACS Med Chem Lett (2017) 8: 1002-1006 [PMID:29057041]
ChEMBL Modulation of gamma secretase in HEK293 cells transfected with human APP with Swedish and London familial AD mutation assessed as reduction in Abeta42 levels incubated for 5 hrs by sandwich immuno-assay B 7.19 pIC50 64 nM IC50 J Med Chem (2020) 63: 8216-8230 [PMID:32786237]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells by sandwich immunoassay B 7.19 pIC50 64 nM IC50 Bioorg Med Chem Lett (2011) 21: 664-669 [PMID:21195610]
ChEMBL Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta42 production after 5 hrs by sandwich immunoassay B 7.19 pIC50 64 nM IC50 J Med Chem (2012) 55: 489-502 [PMID:22098494]
ChEMBL Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells B 7.19 pIC50 64 nM IC50 Bioorg Med Chem Lett (2010) 20: 5380-5384 [PMID:20724152]
ChEMBL Modulation of human gamma-secretase assessed as inhibition of amyloid beta (1 to 42 residues) production by ELISA B 7.08 pEC50 83 nM EC50 J Med Chem (2016) 59: 7389-7409 [PMID:27007185]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by cell based voltage clamp assay B 5.92 pIC50 1200 nM IC50 J Med Chem (2012) 55: 489-502 [PMID:22098494]

ChEMBL data shown on this page come from version 33:

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]