nirogacestat [Ligand Id: 7746] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1770916 (Nirogacestat, PF 03084014, PF-03084014, PF 3084014, PF-3084014) |
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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 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]
