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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 6 hits in this display   

TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM429684(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)
Affinity DataIC50:  75nMAssay Description:The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID NO: 2) by rnADAMTS-5 (1-564-6H).For the d...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM429684(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)
Affinity DataIC50:  75nMAssay Description: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 the dose res...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM429684(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)
Affinity DataIC50:  75nMAssay Description:The basis for the assay is the cleavage of the substrate 520 MMP FRET substrate XII by human ADAMTS6.The substrate contains sequence Arg-Pro-Lys-Pro-...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDisintegrin and metalloproteinase domain-containing protein 17(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM429684(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)
Affinity DataIC50: >100nMAssay Description: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 SYSTEMS INC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCollagenase 3(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM429684(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)
Affinity DataIC50: >100nMAssay Description: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#CC068).For th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM429684(5-cyclopropyl- 5-(3-(4-(3,5- dichlorophenyl) piper...)
Affinity DataIC50:  124nMAssay Description:Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 by biochemical assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed