BDBM143219 US8940748, 26::US9029362, 26::US9687494, 26

SMILES CN1C(=N)N[C@@](C)(CS1(=O)=O)c1cc(NC(=O)c2ccc(cn2)C(F)(F)F)ccc1F

InChI Key InChIKey=XBJQDMHXDUQMJV-UHFFFAOYSA-N

Data  6 KI

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 143219   

TargetBeta-secretase 1(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143219(US8940748, 26 | US9029362, 26 | US9687494, 26)
Affinity DataKi:  1.26nMpH: 5.01Assay Description:The protocol that was used to determine the recited values isdescribed as follows.BACE1 HTRF FRET AssayReagentsNa+-Acetate pH 5.01% Brij-35GlycerolDi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/16/2015
Entry Details
Go to US Patent

TargetBeta-secretase 1(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143219(US8940748, 26 | US9029362, 26 | US9687494, 26)
Affinity DataKi:  1.26nM ΔG°:  -12.3kcal/molepH: 5.0 T: 2°CAssay Description:A homogeneous time-resolved FRET assay was used to determine IC50 values for inhibitors of the soluble human BACE1 catalytic domain. This assay monit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/23/2015
Entry Details
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TargetBeta-secretase 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143219(US8940748, 26 | US9029362, 26 | US9687494, 26)
Affinity DataKi:  2.46nM ΔG°:  -11.9kcal/molepH: 5.0 T: 2°CAssay Description:Inhibitor IC50s at purified human autoBACE-2 were determined in a time-resolved endpoint proteolysis assay that measures hydrolysis of the QSY7-EISEV...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/16/2015
Entry Details
Go to US Patent

TargetBeta-secretase 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143219(US8940748, 26 | US9029362, 26 | US9687494, 26)
Affinity DataKi:  2.46nM ΔG°:  -11.9kcal/molepH: 5.0 T: 2°CAssay Description:Inhibitor IC50s at purified human autoBACE-2 were determined in a time-resolved endpoint proteolysis assay that measures hydrolysis of the QSY7-EISEV...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/23/2015
Entry Details
Go to US Patent

TargetBeta-secretase 1(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143219(US8940748, 26 | US9029362, 26 | US9687494, 26)
Affinity DataKi:  1.26E+3nMpH: 5.0Assay Description:This assay monitored the increase of 620 nm fluorescence that resulted from BACE1 cleavage of an APPswedish APPswe mutant peptide FRET substrate (QSY...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2018
Entry Details
Go to US Patent

TargetBeta-secretase 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143219(US8940748, 26 | US9029362, 26 | US9687494, 26)
Affinity DataKi:  2.46E+3nMpH: 5.0Assay Description:This assay monitored the increase of 620 nm fluorescence that resulted from BACE1 cleavage of an APPswedish APPswe mutant peptide FRET substrate (QSY...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2018
Entry Details
Go to US Patent