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

Found 8 hits in this display   

TargetMucosa-associated lymphoid tissue lymphoma translocation protein 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50:  0.00400nMAssay Description:IC50 values of test compounds were determined with an enzyme activity assay using the C-domain of MALT1 (amino acids 329-824). The readout parameter ...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50:  0.00400nMAssay Description:The assay employs a short peptide substrate labeled with the single fluorophore PT14 as a fluorescence lifetime probe sensitive to the cleavage state...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMucosa-associated lymphoid tissue lymphoma translocation protein 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50:  4nMAssay Description:Inhibition of MALT1 (unknown origin) using Ac-Trp-Leu-Arg-Ser-Arg^Cys(PT14)-NH2 as substrate preincubated for 60 mins followed by substrate addition ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMucosa-associated lymphoid tissue lymphoma translocation protein 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50:  40nMAssay Description:Inhibition of MALT1 in PMA-stimulated human Jurkat T cells assessed as reduction in IL2 level pretreated for 30 mins followed by PMA-stimulation meas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMucosa-associated lymphoid tissue lymphoma translocation protein 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50:  800nMAssay Description:Inhibition of MALT1 in human whole blood assessed as reduction in PMA//anti-CD28 antibody-induced IL2 level pre-incubated for 1 hrs before stimulatio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM355878((S)-1-(2-chloro-7-(1-methoxyethyl)pyrazolo[1,5-a]p...)
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed