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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 beta40 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 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-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] |
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] |
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 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 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]