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ChEMBL ligand: CHEMBL520733 (LY-450139, LY450139, Semagacestat) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as effect on Abeta40 level after 24 hrs by DELFIA | B | 6.7 | pIC50 | 199.53 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1306-1311 [PMID:20056541] |
ChEMBL | Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as decrease in Abeta42 level after 24 hrs by DELFIA | B | 6.9 | pIC50 | 125.89 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1306-1311 [PMID:20056541] |
ChEMBL | Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as decrease in total Abeta level after 24 hrs by DELFIA | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1306-1311 [PMID:20056541] |
ChEMBL | Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as amyloid beta42 formation by ELISA | B | 7.4 | pIC50 | 39.81 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1306-1311 [PMID:20056541] |
ChEMBL | Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as amyloid beta40 formation by ELISA | B | 7.4 | pIC50 | 39.81 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1306-1311 [PMID:20056541] |
ChEMBL | Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2009) 52: 6169-6188 [PMID:19694467] |
ChEMBL | Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2009) 52: 6169-6188 [PMID:19694467] |
GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2009) 52: 6169-88 [PMID:19694467] |
ChEMBL | Inhibition of gamma secretase (unknown origin) mediated Notch signaling | B | 7.85 | pIC50 | 14.1 | nM | IC50 | J Med Chem (2016) 59: 7719-7737 [PMID:27045975] |
ChEMBL | Inhibition of gamma secretase (unknown origin) | B | 7.96 | pIC50 | 10.9 | nM | IC50 | J Med Chem (2016) 59: 7719-7737 [PMID:27045975] |
ChEMBL | Inhibition of gamma-secretase in human H4 cells assessed as reduction in amyloid beta 42 | B | 7.96 | pIC50 | 10.9 | nM | IC50 | Eur J Med Chem (2022) 232: 114169-114169 [PMID:35176561] |
ChEMBL | Inhibition of partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein measured after overnight incubation by ELISA | B | 8.1 | pIC50 | 7.9 | nM | IC50 | J Med Chem (2013) 56: 5261-5274 [PMID:23713656] |
ChEMBL | Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA | B | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2013) 56: 5261-5274 [PMID:23713656] |
ChEMBL | Inhibition of gamma-secretase in human SHSY5Y cells expressing human recombinant APP assessed as increase in Abeta38 level after 24 hrs by DELFIA | B | 6.9 | pEC50 | 125.89 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1306-1311 [PMID:20056541] |
ChEMBL data shown on this page come from version 34:
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]