Compound name
MRK-560
Protein family
Protease
Target name
PSEN1@Protease
Affinity biochemical (nM)
0.65
CG-Set
Protease set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000750a
SMILES
O=S([C@]1(C2=C(C=CC(F)=C2)F)CC[C@H](NS(C(F)(F)F)(=O)=O)CC1)(C3=CC=C(Cl)C=C3)=O
InChIKey
WDZVWDXOIGQJIO-UJKQEGAGSA-N
NCBI gene ID
5663
UniProt ID
P49768
Synonyms
ACNINV3, AD3, FAD, PS-1, PS1, S182
Mode of action
Inhibitor
Negative control
GSI-NC
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radioligand binding assay for APP as target
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/MRK-560
Affinity biochemical relation
=
Selectivity platform
Enzyme and Receptor panel (MSD Pharma/Taiwan)
Selectivity platform number of targets
171
Selectivity remarks
No near family aspartyl proteases detected, closest target: IC50(SLC18A2) = 213 nM, 6 additional targets between 2-10 µM; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: CIT (0%), EGFR (0%), IKBKE (0%), LATS2 (0%), AKT1 (5%), PIK3CA(C420R) (36%); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest target: Ki(SLC6A3) = 3137 nM;
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/MRK-560
Selectivity Number of Off-targets
0