ChEMBL ligand: CHEMBL463981 (Begacestat, GSI-953)
presenilin 1/presenilin 2/Gamma-secretase in Human [ChEMBL: CHEMBL2094135] [GtoPdb: 2402, 2403] [UniProtKB: P49768, P49810, Q8WW43, Q92542, Q96BI3, Q9NZ42] There should be some charts here, you may need to enable JavaScript!

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 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]