EC Number   |
IC50 Value |
IC50 Value Maximum |
Inhibitor |
Reference |
|---|
   3.4.23.46 | -999 |
- |
more |
beta-secretase inhibitors with a hydroxymethylcarbonyl (HMC) isostere used as a substrate transition-state mimic, potent BACE1 inhibitory activities of about 0.0012 mM IC50 shown, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized |
683248 |
| 3.4.23.46 | 0.0000007 |
- |
(S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5H-spiro[chromeno[2,3-b]pyridine-5,4-oxazol]-2-amine |
pH not specified in the publication, temperature not specified in the publication |
734456 |
| 3.4.23.46 | 0.0000009 |
- |
(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 |
pH not specified in the publication, temperature not specified in the publication |
734456 |
| 3.4.23.46 | 0.000001 |
- |
(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 |
pH and temperature not specified in the publication |
711429 |
| 3.4.23.46 | 0.000001 |
- |
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]pyridine-2-carboxamide |
pH and temperature not specified in the publication |
713038 |
| 3.4.23.46 | 0.000001 |
- |
N-[(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-2-oxo-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-19-yl]-N-methylpropane-1-sulfonamide |
pH and temperature not specified in the publication |
711429 |
| 3.4.23.46 | 0.0000012 |
- |
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide |
0.0002 mM, complete inhibition, IC50: 1.2 nM |
667974 |
| 3.4.23.46 | 0.0000012 |
- |
3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-[1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl]leucinamide |
- |
700482 |
| 3.4.23.46 | 0.0000014 |
- |
EVNLAAEF |
Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000014 mM |
669928 |
| 3.4.23.46 | 0.0000016 |
- |
EVNLAAEF |
Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000016 mM |
669928 |
