nirogacestat [Ligand Id: 7746] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1770916 (PF-3084014, PF 03084014, PF-03084014, PF 3084014, Nirogacestat)
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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 human gamma-secretase B 8.21 pIC50 6.2 nM IC50 Eur J Med Chem (2018) 148: 436-452 [PMID:29477076]
ChEMBL Inhibition of gamma secretase isolated from human HeLa cell derived P2 membrane assessed as reduction in amyloid beta (1 to 40 residues) using recombinant human APP-C100 as substrate by DELFIA-based immunoassay B 8.21 pIC50 6.2 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]
ChEMBL Inhibition of human gamma-secretase by cell based assay B 8.89 pIC50 1.3 nM IC50 Eur J Med Chem (2018) 148: 436-452 [PMID:29477076]
ChEMBL Inhibition of gamma-secretase in human H4 cells expressing APP Swedish mutant assessed as inhibition of amyloid beta (1 to 40) production by whole cell assay B 8.92 pIC50 1.2 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 2637-2640 [PMID:21269827]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]