Compile Data Set for Download or QSAR
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 151 hits in this display   

TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of PARP-2 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  0.450nMAssay 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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of N-terminal GST-tagged human PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells using histone mixture (H2A and H2B) a...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of PARP1 (unknown origin) using biotinylated NAD+ as substrate by microplate reader methodMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  0.630nMAssay Description:Inhibition of PARP-1 derived from human HeLa cell nucleusMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  0.730nMAssay Description:Inhibition of PARP-1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of N-terminal GST-tagged human full length PARP1 (2 to 1041 residues) expressed in baculovirus infected Sf9 cells using histone mixture (H...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:Inhibition of PARP-1 (unknown origin) using biotinylated NAD+ as substrate incubated for 45 mins in the presence of deoxy-oligonucleotide by micropla...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Mus musculus (Mouse))
Kudos Pharmaceuticals

LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:A FlashPlate scintillation proximity assay has been used to identify inhibitors of PARP-2. PARP-2 protein (recombinant) was bound down by a PARP-2 sp...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human PARP2 using histone as substrate after 1 hr in presence of biotinylated NAD+ by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1nMAssay Description:Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of recombinant human full-length PARP-2 using biotinylated substrateMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of PARP1 (unknown origin) using biotin-NAD+ as substrate incubated for 1 hr by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of full length recombinant human His6-tagged PARP1 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylat...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of PARP-1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of PARP1 in human G7 cells incubated for 60 mins by immunofluorescence assayMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of PARP1 in human T98G cells incubated for 60 mins by immunofluorescence assayMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of recombinant human PARP-2 expressed in Escherichia coli BL21 (DE3) using sheared DNA as substrate in presence of biotinylated NAD after ...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of recombinant human full length N-terminal GST- tagged PARP1 expressed in baculovirus infected sf9 cells using Colorimetric HRP as substr...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of human PARP1 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysisMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of PARP-2 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of recombinant human PARP1 using NAD+ as substrate incubated for 1 hr by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of recombinant human PARP1 expressed in Escherichia coli BL21(DE3) using histone as substrate measured after 1 hr in presence of biotinyla...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of recombinant human PARP2 using NAD+ as substrate incubated for 1 hr by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells using biotinylated substr...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  2.90nMAssay Description:Inhibition of PARP-2 (unknown origin) binding to DNA assessed as DNA trapping activityMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant human PARP2 using histone as substrate after 1.5 hr in presence of NAD+ by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by strep...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  3.40nMAssay Description:Inhibition of recombinant human C-terminal His-tagged PARP1 expressed in Sf9 insect cells preincubated for 20 mins in presence of activated DNA follo...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of PARP1 (unknown origin) by colorimetric assayMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of recombinant full length human N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 cells using biotinylated substrate afte...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4nMAssay Description:Binding affinity to PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human recombinant PARP1 after 1 hr by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4.20nMAssay Description:Inhibition of PARP1 was assessed using the Universal Chemiluminescent PARPKit. Luminescence readings were normalized to controls and fit to a sigmoid...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4.20nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4.5nMAssay Description:Inhibition of recombinant human GST-fused PARP-1 expressed in Escherichia coli after 30 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells pre-incubated for 30 mins before add...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5nMAssay Description:Inhibition of recombinant human PARP1 using histone as substrate after 1 hr in presence of biotinylated NAD+ by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5nMAssay Description:A FlashPlate scintillation proximity assay has been developed to identify inhibitors of PARP-1. The mechanism of action of the assay requires the bin...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5.10nMAssay Description:Inhibition of recombinant human full-length PARP-1 using biotinylated substrateMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5.20nMAssay Description:Inhibition of PARP-1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  6nMAssay Description:Inhibition of human PARP1 catalytic activity after 10 mins by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant PARP-1 after 1 hr by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  6nMAssay Description:Binding affinity to PARP1 in human OVCAR8 cells assessed as reduction in [125I]-KX1 binding by gamma counting analysisMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant N-terminal Avi-6His-TEV tagged PARP2 full length expressed in pFastBac expression system incubated for 4 hrs by fluor...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  7nMAssay Description:Inhibition of human recombinant N-terminal 6His-6Lys-TEV tagged PARP1 full length expressed in pFastBac expression system incubated for 4 hrs by fluo...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  7nMAssay Description:Inhibition of PARP-1 (unknown origin) using biotinylated NAD+ as substrate after 60 mins by spectrophotometryMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  8nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  8.10nMAssay Description:Inhibition of recombinant human PARP-1 expressed in Escherichia coli BL21 (DE3) using sheared DNA as substrate in presence of biotinylated NAD after ...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  8.40nMAssay Description:Inhibition of human PARP1 expressed in Escherichia coli incubated for 10 mins by colorimetric assayMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  10nMAssay Description:Inhibition of recombinant human His6-tagged PARP1 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins foll...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  11nMAssay Description:Inhibition of human recombinant PARP1 in presence of NAD+ by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  11nMAssay Description:Inhibition of recombinant human PARP1 using histone as substrate after 1 hr in presence of NAD+ by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  11nMAssay Description:Inhibition of PARP-1 (unknown origin) binding to DNA assessed as DNA trapping activityMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  12nMT: 2°CAssay Description:PARP-1 can catalyze the NAD-dependent addition of poly (ADP-ribose) to adjacent nuclear proteins such as histone. The activity of PARP was determined...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  16nMAssay Description:Inhibition of PARP-1 (unknown origin) assessed as incorporation of biotinylated poly ADP-ribose onto histone proteins by colorimetric analysis in pre...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  18.9nMAssay 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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  19nMAssay Description:Inhibition of PARP1 (unknown origin) by ELISAMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  20nMAssay Description:Inhibition of PARP1 (unknown origin) assessed as reduction in biotinylated poly(ADP-ribose) incorporation on to histone protein by ELISA based colori...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  34nMAssay Description:Inhibition of PARP1 (unknown origin) by colorimetric assayMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  36nMAssay Description:Inhibition of recombinant human full length C-terminal His-tagged PARP1 expressed in Sf9 insect cells preincubated for 15 mins followed by NAD+ addit...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  43nMAssay 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
TargetProtein mono-ADP-ribosyltransferase PARP3(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
In DepthDetails ArticlePubMed
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: <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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: <50nMAssay Description:The HTb-PARP-1 positive clones were obtained using the full-length PARP-1 plasmid, through PCR amplification, enzyme digestion, ligation, and transfo...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  85nMAssay Description:Inhibition of human PARP1More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  86.3nMAssay Description:Based on the preliminary PARP1 inhibition evaluation of compounds at molecular level by ELISA, compounds were further evaluated for their cellular in...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  139nMAssay Description:Inhibition of N-terminal GST-tagged human PARP1 expressed in a Baculovirus infected Sf9 insect cells using biotinylated substrate incubated for 1 hr ...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  139nMAssay Description:Inhibition of PARP1 (unknown origin) incubated for 30 mins by fluorescence based analysisMore data for this Ligand-Target Pair
TargetProtein mono-ADP-ribosyltransferase PARP3(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  229nMAssay Description:Inhibition of full length recombinant human His6-tagged PARP3 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP3(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  230nMAssay Description:Inhibition of full length recombinant human His6-tagged PARP3 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  251nMAssay Description:Inhibition of recombinant human His6-tagged PARP2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins foll...More data for this Ligand-Target Pair
TargetProtein mono-ADP-ribosyltransferase PARP3 [R100H](Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
In DepthDetails US Patent
TargetProtein mono-ADP-ribosyltransferase PARP4(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  407nMAssay 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
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP4(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
In DepthDetails ArticlePubMed
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.20E+3nMAssay Description:Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected sf9 cells using histone as substrate after 1...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetProtein mono-ADP-ribosyltransferase PARP10(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.25E+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
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP10(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
In DepthDetails ArticlePubMed
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.26E+3nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.50E+3nMAssay Description:An AlphaScreen (Perkin-Elmer) assay was developed in which His-tagged recombinant TANK-1 protein was incubated with biotinylated NAD+ in a 384-well P...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.57E+3nMAssay Description:Inhibition of TNKS1 (unknown origin) using biotin-NAD+ as substrate incubated for 1 hr in the presence of deoxy-oligonucleotide by ELISA analysis rel...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.70E+3nMAssay Description:Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by st...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected sf9 cells using histone as substrate after ...More data for this Ligand-Target Pair
TargetProtein mono-ADP-ribosyltransferase PARP6(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.90E+3nMAssay Description:Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by s...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  2.96E+3nMAssay Description:Inhibition of human recombinant GST-tagged PARP-1 expressed in Escherichia coli assessed as reduction in NAD+-dependent ADP ribosylation incubated fo...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1/tankyrase-2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: >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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: <3.91E+3nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged PARP-2 expressed in Baculovirus infected Sf9 cells assessed as reduction in NAD+-dependent ADP ...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  4.09E+3nMAssay Description:Inhibition of TNKS2 (unknown origin) using biotin-NAD+ as substrate incubated for 1 hr in the presence of deoxy-oligonucleotide by ELISA analysis rel...More data for this Ligand-Target Pair
TargetProtein mono-ADP-ribosyltransferase PARP16(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5.10E+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
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP16(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
In DepthDetails ArticlePubMed
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  5.77E+3nMAssay Description:Inhibition of PARP1 (unknown origin) incubated for 1 hrs by colorimetric analysisMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  7.09E+3nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
TargetProtein mono-ADP-ribosyltransferase PARP10(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  9.30E+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
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP10(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  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
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP12(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.01E+4nMAssay Description:Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins fol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP12(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.02E+4nMAssay Description:Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins fol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP15(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.76E+4nMAssay Description:Inhibition of recombinant human His6-tagged PARP15 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins fol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein mono-ADP-ribosyltransferase PARP15(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50:  1.78E+4nMAssay Description:Inhibition of recombinant human His6-tagged PARP15 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins fol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: >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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataEC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataEC50:  1.60E+4nMAssay Description:Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assayMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  0.240nMAssay Description:Binding affinity to recombinant human HisGST-tagged PARP-1 catalytic domain by surface plasmon resonance analysisMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  0.280nMAssay Description:Binding affinity to recombinant human HisGST-tagged PARP-2 catalytic domain by surface plasmon resonance analysisMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataEC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataEC50:  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
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataEC50:  16nMAssay Description:Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 0.5 hrs by fluorescenc...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataEC50:  0.400nMAssay Description:Inhibition of PARP-1 in human HeLa cells incubated for 18 hrs in presence of H2O2More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  0.310nMAssay Description:Binding affinity to recombinant human PARP-1 by SPR analysisMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  0.270nMAssay Description:Binding affinity to recombinant human PARP-2 by SPR analysisMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  5.31E+3nMAssay Description:Binding affinity to human GST-tagged PARP-1 ART domain (788 to 1014 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation const...More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 1(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  0.800nMAssay Description:Binding affinity to PARP1 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  0.5nMAssay Description:Binding affinity to PARP2 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
TargetProtein mono-ADP-ribosyltransferase PARP3(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  5.80nMAssay Description:Binding affinity to PARP3 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProtein mono-ADP-ribosyltransferase PARP4(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  141nMAssay Description:Binding affinity to PARP4 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProtein mono-ADP-ribosyltransferase PARP8(Homo sapiens)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to PARP8 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProtein mono-ADP-ribosyltransferase PARP10(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd:  9.70E+3nMAssay Description:Binding affinity to PARP10 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProtein mono-ADP-ribosyltransferase PARP16(Homo sapiens (Human))
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to PARP16 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
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