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

Found 14 hits in this display   

TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50:  40nMAssay Description:ADAMTS-5:Protocol 2: 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 ADAMT...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
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50:  43nMAssay 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
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379646(US9926281, Compound 168)
Affinity DataIC50:  76nMAssay Description:ADAMTS-5:Protocol 2: 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 ADAMT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetADAMTS5(Rattus norvegicus (Rat))
Galapagos

US Patent
LigandPNGBDBM379646(US9926281, Compound 168)
Affinity DataIC50:  129nMAssay Description:ADAMTS-4: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 ADAMTS4For the do...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetA disintegrin and metalloproteinase with thrombospondin motifs 4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50:  635nMAssay Description:Inhibition of human recombinant ADAMTS-4 (AA1 to 520) assessed as cleavage of fluorescent substrate using as TBIS-1 substrate incubated for 180 mins ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target72 kDa type IV collagenase(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379646(US9926281, Compound 168)
Affinity DataIC50:  1.41E+3nMAssay Description:MMP2: Protocol 2: The basis for the assay is the cleavage of the substrate 390 MMP FRET substrate I (Anaspec, Catalog n#: AS-27076) by human MMP2 (R&...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
Target72 kDa type IV collagenase(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50:  2.05E+3nMAssay Description:MMP2: Protocol 2: The basis for the assay is the cleavage of the substrate 390 MMP FRET substrate I (Anaspec, Catalog n#: AS-27076) by human MMP2 (R&...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMatrix metalloproteinase-14(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50:  2.05E+3nMAssay Description:MMP-14:The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat # AS-27076) by human MMP14 (Biomol, Cat #SE-259...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCollagenase 3(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50: >4.00E+3nMAssay Description:MMP-13: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 #CC06...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
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50: >4.00E+3nMAssay Description:TACE: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 SYSTEM...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
LigandPNGBDBM379646(US9926281, Compound 168)
Affinity DataIC50: >2.00E+4nMAssay Description:TACE: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 SYSTEM...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCollagenase 3(Homo sapiens (Human))
Galapagos

US Patent
LigandPNGBDBM379646(US9926281, Compound 168)
Affinity DataIC50: >2.00E+4nMAssay Description:MMP-13: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 #CC06...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 3A4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrateMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM379932(US9926281, Compound 414)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrateMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed