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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]