Information on EC 3.4.23.46 - memapsin 2

Word Map on EC 3.4.23.46
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Specify your search results
Select one or more organisms in this record:
Show additional data
Do not include text mining results
Include (text mining) results (more...)
Include results (AMENDA + additional results, but less precise; more...)

The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.23.46
-
RECOMMENDED NAME
GeneOntology No.
memapsin 2
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
broad endopeptidase specificity. Cleaves Glu-Val-Asn-Leu-/-Asp-Ala-Glu-Phe in the Swedish variant of Alzheimer's amyloid precursor protein
show the reaction diagram
CAS REGISTRY NUMBER
COMMENTARY hide
158736-49-3
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
bat
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
BalbC mice
SwissProt
Manually annotated by BRENDA team
-
1050523 A+, 1084718 A+, 1088995 A+, 1099213 A+, 1131389 A+, 1132960 A+, 1140277 A+, 1155613 A+, 1155622 A+, 1155636 A+, 1155637 A+, 1155641 A+, 1155644 A+, 1155678 A+, 1155687 A+, 1155733 A+, 1155734 A+, 1155765 A+, 1155766 A+, 1155767 A+, 1155771 A+, 1155778 A+, 1155784 A+, 1155786 A+, 1155787 A+, 1155792 A+, 1155797 A+, 1155798 A+, 1155801 A+, 1155803 A+, 1155806 A+, 1155807 A+, 1155809 A+, 1155810 A+, 1155813 A+, 1155830 A+, 1155832 A+, 1155834 A+, 1155841 A+, 1155842 A+, 1155852 A+, 1155853 A+, 1155855 A+, 1155860 A+, 1155863 A+, 1155866 A+, 1155867 A+, 1155869 A+, 1155890 A+, 1155891 A+, 1155897 A+, 1155898 A+, 1155899 A+, 1155915 A+, 1155918 A+, 1155926 A+, 1155929 A+, 1155936 A+, 1155954 A+, 1155959 A+, 1155961 A+, 1155963 A+, 1155965 A+, 1155976 A+, 1155984 A+, 1155985 A+, 1155986 A+, 1155993 A+, 1155998 A+, 1156001 A+, 1156003 A+, 1156009 A+, 1156042 A+, 1156043 A+, 1156047 A+, 1156057 A+, 1156059 A+, 1156060 A+, 1156062 A+, 1156075 A+, 1156076 A+, 1156089 A+, 1156091 A+, 1156101 A+, 1156108 A+, 1156118 A+, 1156119 A+, 1156122 A+, 1156124 A+, 1156125 A+, 1156127 A+, 1156132 A+, 1156134 A+, 1156142 A+, 1156143 A+, 1156149 A+, 1156155 A+, 1156160 A+, 1156161 A+, 1186772 A+, 1250204 A+, 1275000 A+, 1280033 A+, 1280942 A+, 1281978 A+, 1308807 A+, 1318624 A+, 1319942 A+, 1319959 A+, 1319963 A+, 1319966 A+, 1319989 A+, 1319992 A+, 1356221 A+, 1357815 A+, 1405818 A+, 1405844 A+, 1417712 A+, 1422826 A+, 1451422 A+, 1451473 A+, 1451481 A+, 1518681 A+, 1519004 A+, 1519481 A+, 1541099 A+, 1568594 A+, 1585104 A+, 1594996 A+, 1597739 A+, 1638598 A+, 1639776 A+, 1695853 A+, 1721312 A+, 1800358 A+, 1834842 A+, 1836511 A+, 1837093 A+, 1842194 A+, 1868874 A+, 1890092 A+, 1890372 A+, 1897927 A+, 1927184 A+, 1927214 A+, 1931675 A+, 1934529 A+, 1935139 A+, 1936499 A+, 1936603 A+, 1940908 A+, 1945345 A+, 1948049 A+, 1979150 A+, 1979155 A+, 1979156 A+, 1979172 A+, 1979187 A+, 1979206 A+, 1979210 A+, 1979211 A+, 1979223 A+, 1979238 A+, 1979251 A+, 1979252 A+, 1979264 A+, 1979271 A+, 1979273 A+, 1979276 A+, 1979277 A+, 1979278 A+, 1979281 A+, 1979282 A+, 1979284 A+, 1979292 A+, 1979295 A+, 1979301 A+, 1979308 A+, 1979311 A+, 1979320 A+, 1979329 A+, 1979333 A+, 1979337 A+, 1979338 A+, 1979343 A+, 1979355 A+, 1979357 A+, 1979381 A+, 1979383 A+, 1979385 A+, 1979387 A+, 1979391 A+, 1979392 A+, 1979398 A+, 1979405 A+, 1979406 A+, 1979408 A+, 1979409 A+, 1979410 A+, 1979421 A+, 1979427 A+, 1979430 A+, 1979434 A+, 1979439 A+, 1979450 A+, 1979456 A+, 1979461 A+, 1979463 A+, 1979464 A+, 1979467 A+, 1979471 A+, 1979472 A+, 1979477 A+, 1979480 A+, 1979481 A+, 1979483 A+, 1979488 A+, 1979493 A+, 1979495 A+, 1979496 A+, 1979499 A+, 1979500 A+, 1979501 A+, 1979503 A+, 1979504 A+, 1979506 A+, 1979508 A+, 1979511 A+, 1979515 A+, 1979516 A+, 1979521 A+, 1979532 A+, 1979533 A+, 1979535 A+, 1979539 A+, 1979543 A+, 1979544 A+, 1979549 A+, 1979551 A+, 1979555 A+, 1979570 A+, 1979587 A+, 1979590 A+, 1979593 A+, 1979594 A+, 1979599 A+, 1979602 A+, 1979603 A+, 1979605 A+, 1979614 A+, 1979615 A+, 1979616 A+, 1979620 A+, 1979622 A+, 1979623 A+, 1979625 A+, 1979631 A+, 1979633 A+, 1979636 A+, 1979640 A+, 1979645 A+, 1979648 A+, 1979653 A+, 1979654 A+, 1979667 A+, 2106301 A+, 2107376 A+, 2107385 A+, 2108316 A+, 2148459 A+, 2185326 A+, 2208072 A+, 2227553 A+, 2274502 A+, 2296100 A+, 2311256 A+, 2322383 A+, 2343927 A+, 2343930 A+, 2343932 A+, 2343933 A+, 2343934 A+, 2343946 A+, 2343951 A+, 2343971 A+, 2344068 A+, 2344090 A+, 2344133 A+, 2344174 A+, 2344203 A+, 2344224 A+, 2344241 A+, 2344254 A+, 2344257 A+, 2344266 A+, 2344292 A+, 2344298 A+, 2344312 A+, 2344342 A+, 2344349 A+, 2344389 A+, 2344404 A+, 2344430 A+, 2344432 A+, 2344454 A+, 2344455 A+, 2344474 A+, 2344478 A+, 2344502 A+, 2344503 A+, 2344519 A+, 2344532 A+, 2344533 A+, 2344534 A+, 2344596 A+, 2344599 A+, 2344609 A+, 2344611 A+, 2344617 A+, 2344620 A+, 2344622 A+, 2344623 A+, 2344628 A+, 2344629 A+, 2344652 A+, 2344656 A+, 2344658 A+, 2344687 A+, 2344691 A+, 2344692 A+, 2344698 A+, 2344702 A+, 2344704 A+, 2344705 A+, 2344709 A+, 2344712 A+, 2344716 A+, 2344734 A+, 2344735 A+, 2344736 A+, 2344741 A+, 2344744 A+, 2344765 A+, 2344766 A+, 2344785 A+, 2344786 A+, 2344789 A+, 2344792 A+, 2344798 A+, 2423378 A+, 2426569 A+, 2447988 A+, 2460284 A+, 2543244 A+, 2550331 A+, 2579581 A+, 2580013 A+, 2659068 A+, 2682665 A+, 2713067 A+, 2729211 A+, 2811057 A+, 2836082 A+, 2863145 A+, 2876737 A+, 2894471 A+, 2936579 A+, 2961502 A+, 2963452 A+, 2965490 A+, 2966001 A+, 2970306 A+, 2974541 A+, 2974803 A+, 3007140 A+, 3007224 A+, 3007232 A+, 3007256 A+, 3007278 A+, 3007300 A+, 3007322 A+, 3007350 A+, 3007362 A+, 3007364 A+, 3007400 A+, 3007405 A+, 3007423 A+, 3007427 A+, 3007459 A+, 3007465 A+, 3007476 A+, 3007487 A+, 3007498 A+, 3007504 A+, 3007509 A+, 3007538 A+, 3007554 A+, 3007583 A+, 3007608 A+, 3007613 A+, 3007615 A+, 3007628 A+, 3007635 A+, 3007639 A+, 3007683 A+, 3007685 A+, 3007694 A+, 3007718 A+, 3007732 A+, 3007734 A+, 3007735 A+, 3007751 A+, 3007770 A+, 3007784 A+, 3007786 A+, 3007804 A+, 3007815 A+, 3007820 A+, 3007837 A+, 3007845 A+, 3007856 A+, 3007867 A+, 3007868 A+, 3007875 A+, 3007878 A+, 3007887 A+, 3007896 A+, 669928 A+, 669947 A+, 696978 A+, 697442 A+, 700411 A+, 700447 A+, 700851 A+, 710068 A+, 712012 A+, 733728 A+, 750346 A+, 751523 A+, 765148 A+, 829803 A+, 829842 A+, 848585 A+, 884597 A+, 1155646 A++, 1155655 A++, 1155928 A++, 1155941 A++, 1155942 A++, 1155966 A++, 1156006 A++, 1156022 A++, 1156045 A++, 1156112 A++, 1156115 A++, 1279944 A++, 1451679 A++, 1744322 A++, 1979429 A++, 1979568 A++, 1979571 A++, 2343972 A++, 2343973 A++, 2344392 A++, 2344393 A++, 2344397 A++, 2344496 A++, 2344525 A++, 2344572 A++, 2344589 A++, 2344644 A++, 2344668 A++, 2344717 A++, 2344758 A++, 2656729 A++, 2939882 A++, 2963623 A++, 3007536 A++, 3007696 A++, 683380 A++, 683797 A++, 683908 A++, 683911 A++, 712831 A++, 718021 A++, 734524 A++, 848443 A++, 1156028 A++, 1156140 A++, 1282895 A++, 1375270 A++, 1568816 A++, 1678277 A++, 1915770 A++, 1979624 A++, 2314217 A++, 2344550 A++, 2344645 A++, 2344646 A++, 2344724 A++, 2360233 A++, 2460223 A++, 3007822 A++, 670889 A++, 687646 A++, 711429 A++, 717360 A++, 735167 A++, 829878 A++, 1155680 A+++, 1155735 A+++, 1155777 A+++, 1155788 A+++, 1155793 A+++, 1155800 A+++, 1155819 A+++, 1155833 A+++, 1155836 A+++, 1155849 A+++, 1155854 A+++, 1155871 A+++, 1155873 A+++, 1155887 A+++, 1155919 A+++, 1155934 A+++, 1155943 A+++, 1155967 A+++, 1155988 A+++, 1155989 A+++, 1156016 A+++, 1156026 A+++, 1156034 A+++, 1156037 A+++, 1156048 A+++, 1156052 A+++, 1156054 A+++, 1156064 A+++, 1156080 A+++, 1156088 A+++, 1156121 A+++, 1156136 A+++, 1156137 A+++, 1156153 A+++, 1156156 A+++, 1156163 A+++, 638913 A+++, 1155922 A++++, 1155957 A++++, 1156128 A++++, 1156130 A++++, 711918 A++++, 962565 A++++
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
var. acuta
-
-
Manually annotated by BRENDA team
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
1155634 A+, 1155671 A+, 1155681 A+, 1155682 A+, 1155693 A+, 1155700 A+, 1155704 A+, 1155724 A+, 1155782 A+, 1155789 A+, 1155814 A+, 1155820 A+, 1155825 A+, 1155846 A+, 1155862 A+, 1155875 A+, 1155893 A+, 1155920 A+, 1155930 A+, 1155943 A+, 1155956 A+, 1155983 A+, 1155996 A+, 1156002 A+, 1156024 A+, 1156025 A+, 1156026 A+, 1156033 A+, 1156053 A+, 1156070 A+, 1156095 A+, 1156099 A+, 1156104 A+, 1156120 A+, 1156138 A+, 1156148 A+, 1156151 A+, 1223055 A+, 1279928 A+, 1320030 A+, 1344559 A+, 1519389 A+, 1594243 A+, 1594719 A+, 1835548 A+, 1837220 A+, 1931054 A+, 1936531 A+, 1976133 A+, 1979268 A+, 1979309 A+, 1979367 A+, 1979397 A+, 1979446 A+, 1979465 A+, 1979490 A+, 1979511 A+, 1979530 A+, 1979563 A+, 1979567 A+, 1979585 A+, 1979617 A+, 1979630 A+, 1979644 A+, 1979647 A+, 1979651 A+, 2180438 A+, 2208072 A+, 2310322 A+, 2313784 A+, 2323543 A+, 2327689 A+, 2343934 A+, 2344071 A+, 2344145 A+, 2344341 A+, 2344347 A+, 2344366 A+, 2344390 A+, 2344395 A+, 2344467 A+, 2344485 A+, 2344497 A+, 2344536 A+, 2344559 A+, 2344575 A+, 2344580 A+, 2344581 A+, 2344615 A+, 2344618 A+, 2344643 A+, 2344653 A+, 2344665 A+, 2344675 A+, 2344740 A+, 2344763 A+, 2344767 A+, 2344768 A+, 2427607 A+, 2579581 A+, 2759121 A+, 2939818 A+, 3007100 A+, 3007166 A+, 3007209 A+, 3007358 A+, 3007394 A+, 3007478 A+, 3007633 A+, 3007705 A+, 3007788 A+, 3007812 A+, 3007892 A+, 3007896 A+, 669332 A+, 711093 A+, 713110 A+, 713123 A+, 885317 A+, 1156114 A++, 2344495 A++, 2344501 A++, 2344624 A++, 2344760 A++, 3007745 A++, 700416 A++, 1868925 A++, 1979609 A++, 1979612 A++, 1979635 A++, 2343960 A++, 2577497 A++, 2662744 A++, 2965198 A++, 3007725 A++, 3007802 A++, 717360 A++, 734451 A++, 734456 A++, 1155684 A+++, 1155697 A+++, 1155699 A+++, 1155706 A+++, 1155710 A+++, 1155718 A+++, 1155727 A+++, 1155728 A+++, 1155741 A+++, 1155742 A+++, 1155746 A+++, 1155755 A+++, 1155760 A+++, 1155762 A+++, 1155781 A+++, 1155839 A+++, 1155878 A+++, 1155879 A+++, 1155894 A+++, 1155896 A+++, 1155900 A+++, 1155902 A+++, 1155904 A+++, 1155913 A+++, 1155927 A+++, 1155937 A+++, 1155939 A+++, 1155971 A+++, 1155982 A+++, 1155995 A+++, 1156004 A+++, 1156008 A+++, 1156012 A+++, 1156162 A+++
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
-
-
-
Automatic Mining of ENzyme DAta
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
BACE1 heterozygous deletion rescues conditioned taste aversion memory deficits in 5XFAD mice
metabolism
-
BACE1 is responsible for the first step in the production of the beta-amyloid protein of Alzheimer's disease
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
((7-methoxycoumarin-4-yl)acetyl)-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(2,4-dinitrophenyl) + H2O
((7-methoxycoumarin-4-yl)acetyl)-Ser-Glu-Val-Asn-Leu + Asp-Ala-Glu-Phe-Lys(2,4-dinitrophenyl)
show the reaction diagram
((7-methoxycoumarin-4-yl)acetyl)-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(2,4-dinitrophenyl)-Arg-Arg-NH2 + H2O
((7-methoxycoumarin-4-yl)acetyl)-Ser-Glu-Val-Asn-Leu + Asp-Ala-Glu-Phe-Lys(2,4-dinitrophenyl)-Arg-Arg-NH2
show the reaction diagram
-
synthesis, structure and potencies of beta-secretase BACE1 inhibitors optimized, effects of P4 modification on BACE1 inhibitory activity analyzed
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Arg-Lys-(2,4-dinitrophenyl)-Arg-Arg-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)acetyl-L-Ser-L-Glu-L-Val-L-Asn-L-Leu-L-Asp-L-Ala-L-Glu-L-Phe-L-Lys-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-amido-4-methylcoumarin-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-(Lys-2,4-dinitrophenyl)-OH + H2O
?
show the reaction diagram
-
-
-
-
?
7-amido-4-methylcoumarin-Glu-Val-Lys-Met-Asp-Ala-Glu-Phe-(Lys-2,4-dinitrophenyl)-OH + H2O
?
show the reaction diagram
-
-
-
-
?
7-amido-4-methylcoumarin-SEVNLDAEFRK-(2,4-dinitrophenyl)-RR-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-yl-acetyl-SEVNLDAEFR-(2,4-dinitrophenyl)K-RR + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-yl-SEVNLDAEFK-2,4-dinitrophenyl-RR + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-SEVNLDAEFR-Dpa + H2O
?
show the reaction diagram
amyloid -like PROTEIN 2 + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid beta-precursor protein + H2O
?
show the reaction diagram
amyloid pbeta A4 protein + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
?
show the reaction diagram
amyloid precursor protein + H2O
amyloid beta protein 40 + amyloid beta protein 42
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
amyloid protein 1-42 + ?
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
beta-amyloid peptide 40 + beta-amyloid peptide 42
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
C-terminal fragment + soluble N-terminal fragment APPbeta
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
C-terminal fragment C99 of amyloid precursor protein + ?
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
fragments of amyloid precursor protein
show the reaction diagram
amyloid precursor protein + H2O
neurotrophic soluble amyloid precursor protein + ?
show the reaction diagram
-
-
-
-
?
amyloid precursor protein-DELTANL + H2O
?
show the reaction diagram
-
the Swedish familial mutation in APP (DELTANL) enhances beta-secretase cleavage
-
-
?
amyloid-beta precursor protein + H2O
amyloid-beta protein 40 + amyloid-beta protein 42
show the reaction diagram
-
-
-
-
?
amyloid-beta precursor protein + H2O
fragments of amyloid-beta precursor protein
show the reaction diagram
amyloid-like protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
Arg-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(4-(4-dimethylaminophenylazo)benzoic acid)-Arg
Arg-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Glu-Val-Asn-Leu + Asp-Ala-Glu-Phe-Lys(4-(4-dimethylaminophenylazo)benzoic acid)-Arg
show the reaction diagram
-
i.e. FS-1, cleavage occurs at Leu-Asp bond
-
-
?
Arg-Glu(EDANS)-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(Dabcyl)-Arg + H2O
?
show the reaction diagram
-
-
-
-
?
basigin + H2O
?
show the reaction diagram
-
-
-
-
?
beta subunit of voltage-gated sodium channel + H2O
?
show the reaction diagram
-
-
-
-
?
beta-amyloid precursor protein + H2O
fragments of amyloid precursor protein
show the reaction diagram
beta-amyloid precursor protein + H2O
fragments of beta-amyloid precursor protein
show the reaction diagram
beta-amyloid precursor protein APP + H2O
beta-amyloid protein + beta-amyloid precursor protein pre-peptide
show the reaction diagram
beta-secretase 1 + H2O
?
show the reaction diagram
-
-
-
-
?
beta2 subunit of voltage-gated sodium channel + H2O
?
show the reaction diagram
biotin-GLTNIKTEEISEISYEVEFR-C + H2O
?
show the reaction diagram
-
-
-
-
?
biotin-KTEEISEVNFEVEFR + H2O
biotin-KTEEISEVNF + EVEFR
show the reaction diagram
BMP and activin membrane-bound inhibitor homolog + H2O
?
show the reaction diagram
-
-
-
-
?
cache domain containing 1 + H2O
?
show the reaction diagram
-
-
-
-
?
carboxypeptidase D + H2O
?
show the reaction diagram
-
-
-
-
?
casein-FITC + H2O
?
show the reaction diagram
-
-
-
-
?
cation-independent mannose-6-phosphate receptor + H2O
?
show the reaction diagram
-
-
-
-
?
CD166 antigen + H2O
?
show the reaction diagram
-
-
-
-
?
CD276 antigen + H2O
?
show the reaction diagram
-
-
-
-
?
CD44 + H2O
?
show the reaction diagram
-
-
-
-
?
chondroitin sulfate proteoglycan 4 + H2O
?
show the reaction diagram
-
-
-
-
?
contactin-1 + H2O
?
show the reaction diagram
-
-
-
-
?
contactin-2 + H2O
?
show the reaction diagram
-
substrate is a GPI-anchored cell adhesion molecule
mouse and human contactin-2 are physiological substrates for BACE1. BACE1-mediated contactin-2 cleavage tightly regulates the surface expression of contactin-2 in neuronal cells
-
?
cysteine-rich motor neuron 1 protein + H2O
?
show the reaction diagram
-
-
-
-
?
DABCYL-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-EDANS + H2O
?
show the reaction diagram
desmoglein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
disintegrin and metalloproteinase domain-containing protein 10 + H2O
?
show the reaction diagram
-
-
-
-
?
E-cadherin + H2O
?
show the reaction diagram
-
-
-
-
?
EEISEVKMDAEFRG + H2O
EEISEVKM + DAEFRG
show the reaction diagram
-
-
-
-
?
EEISEVNLDAEFRG + H2O
EEISEVNL + DAEFRG
show the reaction diagram
-
-
-
-
?
ephrin type-A receptor 2 + H2O
?
show the reaction diagram
-
-
-
-
?
ephrin type-A receptor 4 + H2O
?
show the reaction diagram
-
-
-
-
?
ephrin type-A receptor 7 + H2O
?
show the reaction diagram
-
-
-
-
?
ephrin-A5 + H2O
?
show the reaction diagram
-
-
-
-
?
ErbB4 + H2O
?
show the reaction diagram
-
-
-
-
?
glypican-3 + H2O
?
show the reaction diagram
-
-
-
-
?
Golgi apparatus protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
Golgi phosphoprotein 4 + H2O
?
show the reaction diagram
-
-
-
-
?
H-RE(EDANS)EVNLDAEFK(dabcyl)R-OH + H2O
?
show the reaction diagram
-
-
-
-
?
hepatocyte growth factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
HLA class I histocompatibility antigen (combined) + H2O
?
show the reaction diagram
-
-
-
-
?
HTARWHLRAQDLHERSAAQLSLSS + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin-6 receptor beta chain + H2O
?
show the reaction diagram
-
-
-
-
?
Jagged-1 + H2O
?
show the reaction diagram
-
-
-
-
?
Klotho protein + H2O
?
show the reaction diagram
-
-
-
-
?
Kunitz-type protease inhibitor 2 + H2O
?
show the reaction diagram
-
-
-
-
?
leucin-rich repeats and immunoglobulin-like domains protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
leucin-rich repeats and immunoglobulin-like domains protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
leucin-rich repeats and immunoglobulin-like domains protein 3 + H2O
?
show the reaction diagram
-
-
-
-
?
leucine-rich repeat-containing protein 33 + H2O
?
show the reaction diagram
-
-
-
-
?
low density lipoprotein receptor-related protein + H2O
?
show the reaction diagram
-
-
-
-
?
low-density lipoprotein receptor-related protein 11 + H2O
?
show the reaction diagram
-
-
-
-
?
low-density lipoprotein receptor-related protein 4 + H2O
?
show the reaction diagram
-
-
-
-
?
M-2420 peptide + H2O
MCA-Ser-Glu-Val-Asn-Leu + Asp-Ala-Glu-Phe-(N6-dinitrophenylacetyl)Lys-amide
show the reaction diagram
-
cleavage occurs between Leu and Asp
-
-
?
Mca-SEVNLDAEFRK(2,4-dinitrophenyl)RR-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
membrane-bound prostaglandin E2 synthase-2 + H2O
?
show the reaction diagram
-
BACE-1 is involved in the cleavage of membrane-bound prostaglandin E2 synthase-2 in its N-terminal portion, which, in turn, enhances the generation of prostaglandin E2
-
-
?
N-cadherin + H2O
?
show the reaction diagram
-
-
-
-
?
neogenin + H2O
?
show the reaction diagram
-
-
-
-
?
netrin receptor UNC5C + H2O
?
show the reaction diagram
-
-
-
-
?
neuronal cell adhesion molecule 1 + H2O
?
show the reaction diagram
-
-
-
-
?
neuronal cell adhesion molecule L1 + H2O
?
show the reaction diagram
-
-
-
-
?
Notch + H2O
Notch intracellular domain + ?
show the reaction diagram
-
-
-
-
?
Notch protein + H2O
?
show the reaction diagram
-
-
-
-
?
Notch-1 + H2O
?
show the reaction diagram
-
-
-
-
?
oxidized insulin B chain + H2O
?
show the reaction diagram
-
-
-
-
?
panvera peptide + H2O
?
show the reaction diagram
-
-
-
-
?
peptidyl-glycine alpha-amidating monooxygenase + H2O
?
show the reaction diagram
-
-
-
-
?
plexin domain-containing protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
podocalyxin-like protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
poliovirus receptor type I + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin 21 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin 7 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma A11 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma A5 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma A8 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma C3 + H2O
?
show the reaction diagram
-
-
-
-
?
protogenin + H2O
?
show the reaction diagram
-
-
-
-
?
RE(EDANS)EVKMDAEFK(Dabcyl)R-NH2 + H2O
?
show the reaction diagram
-
substrate derived from amyloid beta positions -4 to 4, wild-type, internally fluorescent quenched. Very poor substrate
-
-
?
RE(EDANS)EVNLDAEFK(Dabcyl)R-NH2 + H2O
?
show the reaction diagram
-
substrate derived from amyloid beta positions -4 to 4, Swedish mutation, internally fluorescent quenched
-
-
?
receptor protein tyrosine kinase variant EPHB4V1 + H2O
?
show the reaction diagram
-
-
-
-
?
receptor-type tyrosin-protein phosphatase S + H2O
?
show the reaction diagram
-
-
-
-
?
Rh-EVNLDAEFK-quencher + H2O
?
show the reaction diagram
-
-
-
-
?
rhodamine-EVNLDAEFK-DABCYL + H2O
?
show the reaction diagram
-
-
-
-
?
rhodamine-EVNLDAEFK-Quencher
?
show the reaction diagram
-
FRET oligopeptide substrate
-
-
?
rhodamine-EVNLDAEFK-quencher + H2O
?
show the reaction diagram
rhodamine-EVNLDAEFK-quencher + H2O
rhodamine-EVNL + DAEFK-quencher
show the reaction diagram
-
-
-
-
?
roundabout homolog 1 + H2O
?
show the reaction diagram
-
-
-
-
?
roundabout homolog 2 + H2O
?
show the reaction diagram
-
-
-
-
?
seizure 6-like protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-4B + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-4C + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-6A + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-6D + H2O
?
show the reaction diagram
-
-
-
-
?
SEVKMDAEFR + H2O
SEVKM + DAEFR
show the reaction diagram
-
-
-
-
?
SEVKMDAEFRHDSGYEK-biotin + H2O
?
show the reaction diagram
-
-
-
-
?
SEVNLDAEFR + H2O
SEVNL + DAEFR
show the reaction diagram
-
-
-
-
?
SEVNLDAEFRHDSGYEK-biotin + H2O
?
show the reaction diagram
-
-
-
-
?
sidekick-1 + H2O
?
show the reaction diagram
-
-
-
-
?
sidekick-2 + H2O
?
show the reaction diagram
-
-
-
-
?
sortilin type I + H2O
?
show the reaction diagram
-
-
-
-
?
sortilin-related receptor type I + H2O
?
show the reaction diagram
-
-
-
-
?
ST6Gal I + H2O
?
show the reaction diagram
-
i.e. membrane-bound alpha2,6-sialyltransferase, cleavage occurs between Leu37 and Gln38
-
-
?
Swedish mutation of amyloid precursor protein + H2O
fragments of Swedish mutation of amyloid precursor protein
show the reaction diagram
-
-
-
-
?
Swedish variant of amyloid precursor protein + H2O
?
show the reaction diagram
syndecan-4 + H2O
?
show the reaction diagram
-
-
-
-
?
T-cell immunomodulatory protein + H2O
?
show the reaction diagram
-
-
-
-
?
toll-like receptor 9 + H2O
?
show the reaction diagram
-
-
-
-
?
trans-Golgi network integral membrane protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
transmembrane protein 132A + H2O
?
show the reaction diagram
-
-
-
-
?
tumor necrosis factor receptor superfamily member 21 + H2O
?
show the reaction diagram
-
-
-
-
?
ubiquitin + H2O
?
show the reaction diagram
-
-
-
-
?
vesicular integral-membrane protein VIP36 + H2O
?
show the reaction diagram
-
-
-
-
?
Z-Val-Asn-Leu-7-amido-4-methylcoumarin + H2O
Z-Val-Asn-Leu + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
amyloid -like PROTEIN 2 + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid beta-precursor protein + H2O
?
show the reaction diagram
amyloid pbeta A4 protein + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
?
show the reaction diagram
amyloid precursor protein + H2O
amyloid beta protein 40 + amyloid beta protein 42
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
beta-amyloid peptide 40 + beta-amyloid peptide 42
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
C-terminal fragment + soluble N-terminal fragment APPbeta
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
C-terminal fragment C99 of amyloid precursor protein + ?
show the reaction diagram
-
-
-
-
?
amyloid precursor protein + H2O
fragments of amyloid precursor protein
show the reaction diagram
amyloid precursor protein + H2O
neurotrophic soluble amyloid precursor protein + ?
show the reaction diagram
-
-
-
-
?
amyloid precursor protein-DELTANL + H2O
?
show the reaction diagram
-
the Swedish familial mutation in APP (DELTANL) enhances beta-secretase cleavage
-
-
?
amyloid-beta precursor protein + H2O
amyloid-beta protein 40 + amyloid-beta protein 42
show the reaction diagram
-
-
-
-
?
amyloid-beta precursor protein + H2O
fragments of amyloid-beta precursor protein
show the reaction diagram
amyloid-like protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
basigin + H2O
?
show the reaction diagram
-
-
-
-
?
beta subunit of voltage-gated sodium channel + H2O
?
show the reaction diagram
-
-
-
-
?
beta-amyloid precursor protein + H2O
fragments of amyloid precursor protein
show the reaction diagram
beta-amyloid precursor protein + H2O
fragments of beta-amyloid precursor protein
show the reaction diagram
beta-secretase 1 + H2O
?
show the reaction diagram
-
-
-
-
?
beta2 subunit of voltage-gated sodium channel + H2O
?
show the reaction diagram
BMP and activin membrane-bound inhibitor homolog + H2O
?
show the reaction diagram
-
-
-
-
?
cache domain containing 1 + H2O
?
show the reaction diagram
-
-
-
-
?
carboxypeptidase D + H2O
?
show the reaction diagram
-
-
-
-
?
cation-independent mannose-6-phosphate receptor + H2O
?
show the reaction diagram
-
-
-
-
?
CD166 antigen + H2O
?
show the reaction diagram
-
-
-
-
?
CD276 antigen + H2O
?
show the reaction diagram
-
-
-
-
?
CD44 + H2O
?
show the reaction diagram
-
-
-
-
?
chondroitin sulfate proteoglycan 4 + H2O
?
show the reaction diagram
-
-
-
-
?
contactin-1 + H2O
?
show the reaction diagram
-
-
-
-
?
cysteine-rich motor neuron 1 protein + H2O
?
show the reaction diagram
-
-
-
-
?
desmoglein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
disintegrin and metalloproteinase domain-containing protein 10 + H2O
?
show the reaction diagram
-
-
-
-
?
E-cadherin + H2O
?
show the reaction diagram
-
-
-
-
?
ephrin type-A receptor 2 + H2O
?
show the reaction diagram
-
-
-
-
?
ephrin type-A receptor 4 + H2O
?
show the reaction diagram
-
-
-
-
?
ephrin type-A receptor 7 + H2O
?
show the reaction diagram
-
-
-
-
?
ephrin-A5 + H2O
?
show the reaction diagram
-
-
-
-
?
ErbB4 + H2O
?
show the reaction diagram
-
-
-
-
?
glypican-3 + H2O
?
show the reaction diagram
-
-
-
-
?
Golgi apparatus protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
Golgi phosphoprotein 4 + H2O
?
show the reaction diagram
-
-
-
-
?
hepatocyte growth factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
HLA class I histocompatibility antigen (combined) + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin-6 receptor beta chain + H2O
?
show the reaction diagram
-
-
-
-
?
Jagged-1 + H2O
?
show the reaction diagram
-
-
-
-
?
Klotho protein + H2O
?
show the reaction diagram
-
-
-
-
?
Kunitz-type protease inhibitor 2 + H2O
?
show the reaction diagram
-
-
-
-
?
leucin-rich repeats and immunoglobulin-like domains protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
leucin-rich repeats and immunoglobulin-like domains protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
leucin-rich repeats and immunoglobulin-like domains protein 3 + H2O
?
show the reaction diagram
-
-
-
-
?
leucine-rich repeat-containing protein 33 + H2O
?
show the reaction diagram
-
-
-
-
?
low-density lipoprotein receptor-related protein 11 + H2O
?
show the reaction diagram
-
-
-
-
?
low-density lipoprotein receptor-related protein 4 + H2O
?
show the reaction diagram
-
-
-
-
?
membrane-bound prostaglandin E2 synthase-2 + H2O
?
show the reaction diagram
-
BACE-1 is involved in the cleavage of membrane-bound prostaglandin E2 synthase-2 in its N-terminal portion, which, in turn, enhances the generation of prostaglandin E2
-
-
?
N-cadherin + H2O
?
show the reaction diagram
-
-
-
-
?
neogenin + H2O
?
show the reaction diagram
-
-
-
-
?
netrin receptor UNC5C + H2O
?
show the reaction diagram
-
-
-
-
?
neuronal cell adhesion molecule 1 + H2O
?
show the reaction diagram
-
-
-
-
?
neuronal cell adhesion molecule L1 + H2O
?
show the reaction diagram
-
-
-
-
?
Notch + H2O
Notch intracellular domain + ?
show the reaction diagram
-
-
-
-
?
Notch protein + H2O
?
show the reaction diagram
-
-
-
-
?
Notch-1 + H2O
?
show the reaction diagram
-
-
-
-
?
peptidyl-glycine alpha-amidating monooxygenase + H2O
?
show the reaction diagram
-
-
-
-
?
plexin domain-containing protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
podocalyxin-like protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
poliovirus receptor type I + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin 21 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin 7 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma A11 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma A5 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma A8 + H2O
?
show the reaction diagram
-
-
-
-
?
protocadherin gamma C3 + H2O
?
show the reaction diagram
-
-
-
-
?
protogenin + H2O
?
show the reaction diagram
-
-
-
-
?
receptor protein tyrosine kinase variant EPHB4V1 + H2O
?
show the reaction diagram
-
-
-
-
?
receptor-type tyrosin-protein phosphatase S + H2O
?
show the reaction diagram
-
-
-
-
?
rhodamine-EVNLDAEFK-quencher + H2O
?
show the reaction diagram
-
-
-
-
?
roundabout homolog 1 + H2O
?
show the reaction diagram
-
-
-
-
?
roundabout homolog 2 + H2O
?
show the reaction diagram
-
-
-
-
?
seizure 6-like protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-4B + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-4C + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-6A + H2O
?
show the reaction diagram
-
-
-
-
?
semaphoring-6D + H2O
?
show the reaction diagram
-
-
-
-
?
sidekick-1 + H2O
?
show the reaction diagram
-
-
-
-
?
sidekick-2 + H2O
?
show the reaction diagram
-
-
-
-
?
sortilin type I + H2O
?
show the reaction diagram
-
-
-
-
?
sortilin-related receptor type I + H2O
?
show the reaction diagram
-
-
-
-
?
Swedish mutation of amyloid precursor protein + H2O
fragments of Swedish mutation of amyloid precursor protein
show the reaction diagram
-
-
-
-
?
syndecan-4 + H2O
?
show the reaction diagram
-
-
-
-
?
T-cell immunomodulatory protein + H2O
?
show the reaction diagram
-
-
-
-
?
toll-like receptor 9 + H2O
?
show the reaction diagram
-
-
-
-
?
trans-Golgi network integral membrane protein 2 + H2O
?
show the reaction diagram
-
-
-
-
?
transmembrane protein 132A + H2O
?
show the reaction diagram
-
-
-
-
?
tumor necrosis factor receptor superfamily member 21 + H2O
?
show the reaction diagram
-
-
-
-
?
vesicular integral-membrane protein VIP36 + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cu
-
BACE1 cytoplasmic domain interacts with the copper chaperone for superoxide dismutase-1 and binds copper
Cu2+
-
involvement of aspartic proteinase BACE1 in copper homoeostasis shown, key role of the central of three cysteines (amino acid 482 in 501-amino-acid isoform of BACE1) in metal binding indicated
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+)-byakangelicin
-
-
(+)-byakangelicol
-
-
(+)-oxypeucedanin
-
-
(-)-gallocatechin gallate
-
less potent inhibitor
(13S)-15-amino-10,13-dicyclohexyl-19-fluoro-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(13S)-15-amino-10,13-dicyclohexyl-19-methoxy-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(13S)-15-amino-10,13-dicyclohexyl-2-oxa-10,14,16,19-tetraazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(14S)-16-amino-10,14-dicyclohexyl-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
potent inhibitor
(14S)-16-amino-10-cyclohexyl-14-(propan-2-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(14S)-16-amino-14-(propan-2-yl)-10-(tetrahydro-2H-pyran-4-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(14S)-16-amino-14-cyclohexyl-10-(tetrahydro-2H-pyran-4-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(15R)-17-amino-11,15-dicyclohexyl-2-oxa-11,16,18-triazatetracyclo[14.5.3.1(3,7).0(19,23)]pentacosa-1(21),3(25),4,6,17,19,22-heptaen-12-one
-
-
(15S)-17-amino-11,15-dicyclohexyl-2-oxa-11,16,18-triazatetracyclo[14.5.3.1(3,7).0(19,23)]pentacosa-1(21),3(25),4,6,17,19,22-heptaen-12-one
-
-
(1R,3S)-3-[(1S)-1-(acetylamino)-2-methylpropyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[(1S)-1-(acetylamino)-3-methylbutyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
11% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)butyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
15% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)ethyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
8% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)propyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
17% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)-3-methylbutyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
42% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)butyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
80% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)cyclopentyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[1-(acetylamino)ethyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
14% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)propyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
24% inhibition at 0.01 mM
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopiperidin-1-yl)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopyrrolidin-1-yl)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(propanoylamino)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-[methyl(propanoyl)amino]propan-2-yl]cyclohexanecarboxamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[(1-benzylpiperidin-4-yl)amino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
dual inhibitor of both beta-secretase and acetylcholinesterase, good inhibitory effects on amyloid beta production of amyloid precursor protein transfected HEK293 cells
(1S,2R)-N-{1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl}-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
dual inhibitor of both beta-secretase and acetylcholinesterase. Intracerebroventricular injection of into amyloid precursor protein transgenic mice causes a 29% reduction of amyloid beta1-40 production
(2R,4S)-N-butyl-4-hydroxy-2-methyl-4-[(2S,5S,7R)-1,2,7-trimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]butanamide
-
56fold selectivity for beta-secretase over cathepsin D
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,15-dioxo-1,4-diazacyclopentadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
-
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
-
(2R,4S,5S)-N-benzyl-4-hydroxy-2,7-dimethyl-5-[(N-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-seryl)amino]octanamide
-
16.45% inhibition at 0.01 mg/ml
(2R,4S,5S)-N-benzyl-4-hydroxy-5-([N-[(4-methoxyphenyl)acetyl]-L-seryl]amino)-2,7-dimethyloctanamide
-
25.09% inhibition at 0.01 mg/ml
(2S)-2-((3R)-3-acetamido-3-isobutyl-2-oxo-1-pyrrolidinyl)-N-((1S,2R)-1-(3,5-difluorobenzyl)-2-hydroxy-2-(1,2,3,4-tetrahydro-3-isoquinolinyl)ethyl)-4-phenylbutanamide
-
crystallization data, EC50 value for HEK293 cells 10 nM
(2S)-2-((S)-3-acetamido-3-((R)-sec-butyl)-2-oxopyrrolidin-1-yl)-N-((1S,2S)-3-(3,5-difluorophenyl)-1-hydroxy-1-((2R)-5-(propylsulfonyl)pyrrolidin-2-yl)propan-2-yl)-4-phenylbutanamide
(2S,5S,8S,11S,14S)-14-amino-5-benzyl-8-(cyclohexylmethyl)-16-(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)-2-hydroxy-11-(1-methylethyl)-4,7,10,13,16-pentaoxo-N-[3-(2H-tetrazol-5-yl)phenyl]-3,6,9,12-tetraazahexadecan-1-amide
-
i.e. KMI-574, 100% and 97% inhibition at 2 microM and 0.2 microM, respectively, 84% inhibition of beta-secretase BACE1 in cultured cell-based assay at 100 microM
(3S,14R,16S)-16-[(1R)-1-hydroxy-2-([3-(1-methylethyl)benzyl]amino)ethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
(3S,14R,16S)-16-[(1S)-2-[[(1R)-3,3-dimethyl-7-(1-methylethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]-1-hydroxyethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
(3S,5R)-3-(4-amino-3-fluoro-5-[[(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl]oxy]benzyl)-5-[(3-tert-butylbenzyl)amino]-4-hydroxytetrahydro-2H-thiopyranium-1-olate
-
highly potent, selective inhibitors with improved cellular activity. Sufficient central nervous system exposure can be achieved with a single oral dose of 60 micromol/kg to effect significant reduction in brain amyloid beta in APP51/16 transgenic mice
(4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(fluoromethyl)-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-amine
-
upon oral administration, inhibitor exhibits robust brain availability and is efficacious in lowering central amyloid beta levels in mouse and dog. Chronic treatment in aged PS1/APP mice effects a decrease in the number and size of amyloid-beta-derived plaques. Evaluation of the inhibitor in a 2-week exploratory toxicology study exhibits no accumulation of autofluorescent material in retinal pigment epithelium or histology findings in the eye
(4aS,4'S,10aR)-8-(2-fluoropyridin-3-yl)-4a-methyl-3,4,4a,10a-tetrahydro-2H,5'H-spiro[pyrano[3,2-b]chromene-10,4'-thiazol]-2'-amine
-
compound demonstrates a 69% reduction in rat cerebrospinal fluid amyloid beta1?40 at 60 mg/kg
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(2-oxopyrrolidin-1-yl)-11,16-dioxa-3-azatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(methoxymethyl)-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]ethyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([2-[3-(propan-2-yl)phenyl]propan-2-yl]amino)ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11-oxa-3,16,18-triazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2,2,2-trifluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-fluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-methoxyethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclobutyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclopentyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(5S)-2-amino-5-(2',4'-difluorobiphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
5fold selectivity for BACE2 over BACE1, 27fold selectivity for BACE2 over cathepsin D
(5S)-2-amino-5-[3-fluoro-5-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
(6R)-2,6-anhydro-5-O-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-[2-[(2R)-2-hydroxypropyl]-7-methoxy-5-methyl-4-oxo-4H-chromen-8-yl]-L-glucitol
-
inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 7.4% in B103 neuroblastoma cells at 30 ppm
(6R)-2,6-anhydro-6-[7-methoxy-5-methyl-4-oxo-2-[(1E)-prop-1-en-1-yl]-4H-chromen-8-yl]-L-glucitol
-
inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 12.3% in B103 neuroblastoma cells at 30 ppm
(7S,12Z)-N-[(2S,4R)-2-hydroxy-4-methyl-5-[[(1S)-2-methyl-1-(phenylcarbamoyl)propyl]amino]-1-(2-methylpropyl)-5-oxopentyl]-4-(1-methylethyl)-2,5,9-trioxo-1-oxa-3,6,10-triazacyclohexadec-12-ene-7-carboxamide
-
-
(R)-3-(2-amino-6-(3-chloropyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 80 nM
(R)-3-(2-amino-6-(3-methylpyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 35 nM
(S)-3-(6,6-dimethyl-3,6-dihydro-2H-pyran-4-yl)-7-(2-fluoropyridin-3-yl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine
-
inhibitor shows good BACE1 functional potency, permeability, intrinsic stability, and P-glycoprotein efflux ratios
(S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5H-spiro[chromeno[2,3-b]pyridine-5,4-oxazol]-2-amine
-
i.e. AMG-8718.compound exhibits a balanced profile of BACE1 potency, hERG binding affinity, and P-glycoprotein recognition. Compound produces robust and sustained reductions of cerebrospinal fluid and brain amyloid beta levels in a rat pharmacodynamic model
1,1'-piperazine-1,4-diylbis[3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol]
-
inhibitor identified by in silico mulit-filter approaches. Calculated binding free energy of R,S-isomer -48 kcal/mol
1,1'-piperazine-1,4-diylbis[3-(9H-carbazol-9-yl)propan-2-ol]
-
inhibitor identified by in silico mulit-filter approaches. Calculated binding free energy of S,R-isomer -48.2 kcal/mol
1,3-bis(3,5-bis(trifluoromethyl)phenyl)urea
-
100% inhibition at 100 nM, 15% inhibition at 10 nM
1,5-anhydro-1-[7-hydroxy-2-[(2S)-2-hydroxypropyl]-5-methyl-4-oxo-4H-chromen-8-yl]hexitol
-
37.2% inhibition at 0.1 mM
1,5-anhydro-1-[7-hydroxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]-2-O-[(E)-2-(4-hydroxyphenyl)ethenyl]hexitol
-
39.5% inhibition at 0.1 mM
1,5-anhydro-1-[7-methoxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol
-
41.0% inhibition at 0.1 mM
1,5-anhydro-2-O-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-1-[7-hydroxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol
-
36.4% inhibition at 0.1 mM
1,5-anhydro-2-O-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-1-[7-methoxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol
-
48.7% inhibition at 0.1 mM
1-(2-chlorobenzyl)-4-(4-(dibenzo[b,d]furan-1-yl)benzyl)-1H-imidazol-2-amine
-
0.005 mM, 37.8% inhibition. Inhibitor is predicted to be able to cross the blood-brain barrier
1-(3,5-bis(trifluoromethyl)-phenyl)-3-(3,5-dimethylphenyl)urea
-
80% inhibition at 100 nM
1-(4-fluorobenzyl)-4-((30,50-dimethoxybiphenyl-4-yl)methyl)-1H-imidazol-2-amine
-
0.005 mM, 40% inhibition. Inhibitor is predicted to be able to cross the blood-brain barrier
1-[ (3-benzoylamino-phenylcarbamoyl)-methyl]-pyridinium chloride
-
51% inhibition at 0.05 mM
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-carbamoyl-pyridiniumchloride
-
54% inhibition at 0.05 mM
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
55% inhibition at 0.05 mM
1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
61% inhibition at 0.05 mM
1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
42% inhibition at 0.05 mM
1-[(E)-[(4-methylquinazolin-2-yl)amino][(phenylcarbamoyl)amino]methylidene]-3-phenylurea
-
complete inhibition at 0.1 mM
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
78% inhibition at 0.05 mM
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
44% inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylsulfamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
50% inhibition at 0.05 mM
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
-
11-oxo-N-(pyridin-4-yl)-10,11-dihydro-5H-dibenzo[b,e][1,4]-diazepine-3-carboxamide
-
-
16-amino-11-cyclohexyl-2-oxa-11,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-12-one
-
-
1[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
68% inhibition at 0.05 mM
2'-O-coumaroyl-(S)-aloesinol
-
51.9% inhibition at 0.1 mM
2'-O-[p-methoxy-(E)-cinnamoyl]-(S)-aloesinol
-
34.1% inhibition at 0.1 mM
2,3-dihydro-6-methylginkgetin
-
isolated from from Cephalotaxus harringtonia var. fastigiata
2,3-dihydroamentoflavone
-
a 2,3-dihydroamentoflavone from Cycas revoluta
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
-
i.e. norartocarpetin, prenylated flavone from the stem bark of Morus lhou, noncompetitive
2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole
-
inhibitor of BACE1, EC 3.4.23.46. 150fold more effective on BACE1 than BACE2
2-amino-3,4-dihydroquinazoline
-
-
2-amino-3-ethyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(pyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
exhibits modest selectivity (about 8fold) against BACE2
2-amino-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-5-[3-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-phenyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-[2-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-[2-methyl-6-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
24% inhibition at 0.0125 mM
2-amino-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(1,3-benzodioxol-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2,3-dihydro-1-benzofuran-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2,6-diethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2,6-dimethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2-ethyl-6-methylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
28% inhibition at 0.0125 mM
2-amino-5-(2-ethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3,4-dimethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3-butoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3-ethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3-methoxy-4-methylphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-ethyl-3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-(6-methylbiphenyl-3-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3,4-dimethoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3-butoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3-chloro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3-cyclopentyl-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-propoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3-fluoro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-[3-(cyclopentyloxy)-4-methoxyphenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(propan-2-yloxy)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(trifluoromethyl)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[2-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[3-(2-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[3-(6-fluoropyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[3-(6-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[3-fluoro-5-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[4-fluoro-3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
; aminohydantoin inhibitor, shows comparable activity in a cell-based assay, and demonstrates more than 100fold selectivity for the other structurally related aspartyl proteases BACE2, cathepsinD, renin, and pepsin
2-deoxy-4-O-beta-D-glucopyranuronosyl-6-O-sulfo-2-(sulfoamino)-beta-D-glucopyranose
-
IC50: 0.000053 mg/ml
2-[(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)amino]-2-oxoethyl [(4,6-diphenylpyrimidin-2-yl)sulfanyl]acetate
-
75% inhibition at 0.1 mM
2-[(3-cyano-4,6-diphenylpyridin-2-yl)sulfanyl]-N-(3-nitrophenyl)acetamide
-
complete inhibition at 0.1 mM
2-[(4-methyl-5-[2-[(4-methylphenyl)amino]-2-oxoethyl]-4H-1,2,4-triazol-3-yl)sulfanyl]-N-(4-phenyl-1,3-thiazol-2-yl)acetamide
-
83% inhibition at 0.1 mM
2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]-N-(2-fluorophenyl)acetamide
-
90% inhibition at 0.1 mM
2-[[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]carbamoyl]-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]pyridin-4-yl methanesulfonate
-
i.e. KMI-1036, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
-
-
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol
-
1.7% inhibition at 0.0125 mM
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
-
8.46% inhibition at 0.0125 mM
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol
-
5.43% inhibition at 0.0125 mM
2-[[3-cyano-4-(4-fluorophenyl)-6-phenylpyridin-2-yl]sulfanyl]-N-(tricyclo[3.3.1.1(3,7)]dec-1-yl)acetamide
-
45% inhibition at 0.1 mM
2-[[3-cyano-6-(4-fluorophenyl)-4-phenylpyridin-2-yl]sulfanyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)acetamide
-
80% inhibition at 0.1 mM
2-[[4-(4-chlorophenyl)-3-cyano-6-(4-methoxyphenyl)pyridin-2-yl]sulfanyl]-N-(naphthalen-2-yl)-N-phenylacetamide
-
68% inhibition at 0.1 mM
2-[[4-benzyl-5-(1H-indol-3-ylmethyl)-4H-1,2,4-triazol-3-yl]sulfanyl]-1-(1H-indol-3-yl)ethanone
-
75% inhibition at 0.1 mM
3-(3H-imidazo[4,5-c]pyridin-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(5-((7aR)-6-(5-fluoropyrimidin-2-yl)-2-imino-3-methyl-4-oxooctahydro-1H-pyrrolo[3,4-d]pyrimidin-7a-yl)thiophen-3-yl)benzonitrile
-
orally active, brain penetrant inhibitor that reduces amyloid beta40 in the plasma, cerebrospinal fluid, and cortex of rats in a dose-dependent manner
3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(5-(pyridin-4-yl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]-diazepin-11(10H)-one
-
-
3-(6-(2-acetylphenyl)-2-aminoquinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 11 nM
3-(6-fluoro-1H-benzo[d]imidazol-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(benzylsulfanyl)-6-(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
-
48% inhibition at 0.1 mM
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(3,3,3-trifluoropropanoyl)-D-alaninamide
-
-