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] |
| Gamma-secretase-activating protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638343] [UniProtKB: A4D1B5] | ||||||||
| ChEMBL | Inhibition of human gamma secretase by western blot assay | B | 8.21 | pIC50 | 6.2 | nM | IC50 | J Med Chem (2021) 64: 2382-2418 [PMID:33650861] |
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]
