DAPT [Ligand Id: 11363] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL255682
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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 Displacement of [3H]L685458 from gamma-secretase in human THP1 cells B 4 pIC50 >100000 nM IC50 J Biol Chem (2007) 282: 36829-36836 [PMID:17932033]
ChEMBL Inhibition of gamma secretase (unknown origin) mediated Notch signaling by cell based luciferase reporter gene assay B 6.3 pIC50 500 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]
ChEMBL Inhibition of gamma secretase in human primary neuronal cells assessed as reduction in amyloid beta 40 B 6.94 pIC50 115 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]
ChEMBL Displacement of [3H]IN973 from gamma-secretase in human THP1 cells B 8.2 pIC50 6.3 nM IC50 J Biol Chem (2007) 282: 36829-36836 [PMID:17932033]

ChEMBL data shown on this page come from version 35:

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]