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 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]