Literature summary for 3.4.23.46 extracted from

Yang, H.C.; Chai, X.; Mosior, M.; Kohn, W.; Boggs, L.N.; Erickson, J.A.; McClure, D.B.; Yeh, W.K.; Zhang, L.; Gonzalez-DeWhitt, P.; Mayer, J.P.; Martin, J.A.; Hu, J.; Chen, S.H.; Bueno, A.B.; Little, S.P.; McCarthy, J.R.; May, P.C.
Biochemical and kinetic characterization of BACE1: investigation into the putative species-specificity for beta- and beta-cleavage sites by human and murine BACE1 (2004), J. Neurochem., 91, 1249-1259.

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Inhibitors

Inhibitors	Comment	Organism
EVD(statine)VAEF	IC50: 0.000651 mM	Homo sapiens
EVD(statine)VAEF	IC50: 0.000603 mM	Mus musculus
EVE(statine)VAEF	IC50: 0.00045 mM	Homo sapiens
EVE(statine)VAEF	IC50: 0.000452 mM	Mus musculus
EVG(statine)VAEF	IC50: 0.005319 mM	Homo sapiens
EVG(statine)VAEF	IC50: 0.004673 mM	Mus musculus
EVL(statine)VAEF	IC50: 0.000265 mM	Homo sapiens
EVL(statine)VAEF	IC50: 0.000251 mM	Mus musculus
EVNLAAEF	Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000016 mM	Homo sapiens
EVNLAAEF	Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000014 mM	Mus musculus
EVW(statine)VAEF	IC50: 0.00754 mM	Homo sapiens
EVW(statine)VAEF	IC50: 0.0066 mM	Mus musculus
EVY(statine)VAEF	IC50: 0.000118 mM	Homo sapiens
EVY(statine)VAEF	IC50: 0.000126 mM	Mus musculus
KTEEISEVN(statine)VAEF	0.000055 mM	Homo sapiens
KTEEISEVN(statine)VAEF	0.000049 mM	Mus musculus
LY2039911	-	Homo sapiens
LY2039911	-	Mus musculus
additional information	murine BACE1 in amyloid precursor protein transgenic mouse models should exhibit similar pharmacological and enzymatic profiles to those of human BACE1 and should thus be useful in the development of BACE inhibitors for the treatment of Alzheimer's disease	Homo sapiens
additional information	murine BACE1 in amyloid precursor protein transgenic mouse models should exhibit similar pharmacological and enzymatic profiles to those of human BACE1 and should thus be useful in the development of BACE inhibitors for the treatment of Alzheimer's disease	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Mus musculus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
brain	-	Mus musculus	-
brain	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
amyloid precursor protein + H2O	-	Mus musculus	?	-	?
amyloid precursor protein + H2O	-	Homo sapiens	?	-	?

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.0000014	-	Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000014 mM	Mus musculus	EVNLAAEF
0.0000016	-	Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000016 mM	Homo sapiens	EVNLAAEF
0.000118	-	IC50: 0.000118 mM	Homo sapiens	EVY(statine)VAEF
0.000126	-	IC50: 0.000126 mM	Mus musculus	EVY(statine)VAEF
0.000251	-	IC50: 0.000251 mM	Mus musculus	EVL(statine)VAEF
0.000265	-	IC50: 0.000265 mM	Homo sapiens	EVL(statine)VAEF
0.00045	-	IC50: 0.00045 mM	Homo sapiens	EVE(statine)VAEF
0.000452	-	IC50: 0.000452 mM	Mus musculus	EVE(statine)VAEF
0.000603	-	IC50: 0.000603 mM	Mus musculus	EVD(statine)VAEF
0.000651	-	IC50: 0.000651 mM	Homo sapiens	EVD(statine)VAEF
0.004673	-	IC50: 0.004673 mM	Mus musculus	EVG(statine)VAEF
0.005319	-	IC50: 0.005319 mM	Homo sapiens	EVG(statine)VAEF
0.0066	-	IC50: 0.0066 mM	Mus musculus	EVW(statine)VAEF
0.00754	-	IC50: 0.00754 mM	Homo sapiens	EVW(statine)VAEF