Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 12 hits in this display
BDBM471740((R)-5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) pip...)
BDBM471732(5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) piperaz...)
IC50: 37.5nMAssay Description:TABLE X: The IC50 value for test compounds can be determined in a fluorescent based protease assay.The basis for the assay is the cleavage of the sub...More data for this Ligand-Target Pair
ADAMTS5(Rattus norvegicus (Rat))Galapagos
US Patent
BDBM471732(5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) piperaz...)
BDBM471732(5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) piperaz...)
BDBM471732(5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) piperaz...)
BDBM471740((R)-5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) pip...)
BDBM471732(5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) piperaz...)
BDBM471740((R)-5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) pip...)
IC50: >1.00E+4nMAssay Description:TABLE XI: The basis for the assay is the cleavage of the substrate 5FAM-LAQAVRSSSRK-5TAMRA (SEQ ID NO: 3) (Anaspec, custom 34891) by human TACE (R&D ...More data for this Ligand-Target Pair
BDBM471732(5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) piperaz...)
IC50: >1.00E+4nMAssay Description:TABLE XII: The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat #AS-27076) by human MMP13 (Chemicon, Cat #C...More data for this Ligand-Target Pair
BDBM471740((R)-5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) pip...)
BDBM471732(5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) piperaz...)
IC50: >1.00E+4nMAssay Description:TABLE VI: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by human ADAMTS4.For the...More data for this Ligand-Target Pair
BDBM471740((R)-5-[3-[4-(3,4- difluoro-5- methoxy- phenyl) pip...)
IC50: >1.00E+4nMAssay Description:TABLE IX: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by human ADAMTS-5.For th...More data for this Ligand-Target Pair