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) assessed as inhibition of Amyloid beta 40 production by cell-based assay	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2022) 232: 114169-114169 [PMID:35176561]
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]
ChEMBL	Inhibition of gamma-secretase (unknown origin) assessed as inhibition of Amyloid beta 40 production by cell-free assay	B	7.83	pEC50	14.8	nM	EC50	Eur J Med Chem (2022) 232: 114169-114169 [PMID:35176561]
GtoPdb	-	-	7.83	pEC50	14.8	nM	EC50	J Pharmacol Exp Ther (2009) 331: 598-608 [PMID:19671883]
ChEMBL	Inhibition of gamma-secretase (unknown origin) assessed as inhibition of Amyloid beta 42 production by cell-free assay	B	7.91	pEC50	12.4	nM	EC50	Eur J Med Chem (2022) 232: 114169-114169 [PMID:35176561]

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]