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ChEMBL ligand: CHEMBL463981 (Begacestat, GSI-953) |
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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 (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta42 secretion by ELISA | B | 6.38 | pIC50 | 414 | nM | IC50 | J Med Chem (2013) 56: 1443-1454 [PMID:23342950] |
ChEMBL | Inhibition of gamma secretase (unknown origin) mediated Notch M1726V mutant activation in CHO K1 cells after 48 hrs by chemiluminescence assay | B | 6.68 | pIC50 | 208.5 | nM | IC50 | J Med Chem (2016) 59: 7719-7737 [PMID:27045975] |
ChEMBL | Inhibition of gamma-secretase (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta40 secretion by ELISA | B | 6.69 | pIC50 | 203 | nM | IC50 | J Med Chem (2013) 56: 1443-1454 [PMID:23342950] |
ChEMBL | Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2009) 52: 6169-6188 [PMID:19694467] |
ChEMBL | Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloid beta 40 after 24 hrs by sandwich ELISA | B | 7.83 | pIC50 | 14.8 | nM | IC50 | J Med Chem (2016) 59: 7719-7737 [PMID:27045975] |
ChEMBL | Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2013) 56: 5261-5274 [PMID:23713656] |
ChEMBL | Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA | B | 7.98 | pIC50 | 10.5 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 996-1000 [PMID:23312944] |
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 | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2009) 52: 6169-6188 [PMID:19694467] |
ChEMBL | Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 996-1000 [PMID:23312944] |
ChEMBL | Inhibition of partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein measured after overnight incubation by ELISA | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2013) 56: 5261-5274 [PMID:23713656] |
GtoPdb | - | - | 7.83 | pEC50 | 14.8 | nM | EC50 | J Pharmacol Exp Ther (2009) 331: 598-608 [PMID:19671883] |
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]