Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 151 hits in this display
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 0.400nMAssay Description:Inhibition of PARP-2 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 0.5nMAssay Description:Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate mea...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 0.600nMAssay Description:Inhibition of PARP1 (unknown origin) incubated for 45 mins in presence of biotinylated-NAD+ by microplate reader analysisMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 0.900nMAssay Description:In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compo...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 1.20nMAssay Description:Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured af...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 2.5nMAssay Description:Inhibition of human full length PARP1 expressed in Escherichia coli rosetta (DE3) incubated for 20 mins by fluorescence analysisMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 5.20nMAssay Description:In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compo...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 8nMAssay Description:HT Universal Chemiluminescent PARP Assay Kit with Histone-coated Strip Wells, commercially available from Trevigen (US), Catalog #: 4676-096-K.More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 10nMAssay Description:Inhibition of GST-tagged recombinant human PARP-1 expressed in Escherichia coli after 30 mins by fluorescence-based assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 10.4nMAssay Description:In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compo...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 12nMAssay Description:Inhibition of full length recombinant human His6-tagged PARP2 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylat...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 12nMAssay Description:Inhibition of PARP1 (unknown origin) incubated for 10 mins using biotinylated NAD+ and activated DNA by colorimetric assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 46nMAssay Description:Inhibition of PARP3 (unknown origin) using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: <50nMAssay Description:The HTb-PARP1 positive clones were obtained using the full-length PARP1 plasmid, through PCR amplification, enzyme digestion, ligation, and transform...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 69nMAssay Description:Inhibition of recombinant human His6-tagged PARP1 C-3-zinc finger domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 69.2nMAssay Description:Inhibition of recombinant human His6-tagged PARP1 C-3-zinc finger domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 320nMAssay Description:In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compo...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 410nMAssay Description:Inhibition of recombinant human His6-tagged PARP4 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins foll...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 1.23E+3nMAssay Description:Inhibition of recombinant human TNKS1 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biot...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 1.26E+3nMAssay Description:Inhibition of recombinant human His6-tagged PARP10 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins fol...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 1.70E+3nMAssay Description:In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compo...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 2.34E+3nMAssay Description:Inhibition of recombinant human TNKS2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biot...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: >3.00E+3nMAssay Description:Inhibition of TNSK1/2-activated Wnt pathway in human DLD-1 TOPFlash/EF1a Renilla reporter cells after 24 hrs by Steady-Glo Luciferase assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 5.13E+3nMAssay Description:Inhibition of full length recombinant human His6-tagged PARP16 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinyla...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: 9.33E+3nMAssay Description:Inhibition of full length recombinant human His6-tagged PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinyla...More data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
IC50: >7.00E+4nMAssay Description:Inhibition of human recombinant PARP5a (E1023 to T1327 amino acids) incubated for 4 hrs by fluorescence anisotropy binding assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
EC50: 60nMAssay Description:Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomideMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
EC50: 3.60nMAssay Description:Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
EC50: 2.5nMAssay Description:Inhibition of PARP-1 in human HeLa cells assessed as decrease of H2O2-induced PARylation after 3 hrs by fluorescence assayMore data for this Ligand-Target Pair
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
BDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Displayed 1 to 50 (of 151 total ) | Next | Last >>