null
SMILES Fc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CCN(CC1)C(=O)C1CC1
InChI Key InChIKey=FDLYAMZZIXQODN-UHFFFAOYSA-N
PDB links: 7 PDB IDs match this monomer.
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 151 hits for monomerid = 27566
Affinity DataIC50: 6nMAssay Description:Inhibition of human PARP1 catalytic activity after 10 mins by ELISAMore data for this Ligand-Target Pair
3D Structure (crystal)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
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
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
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
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
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
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
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
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
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 2(Homo sapiens (Human))
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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
TargetProtein mono-ADP-ribosyltransferase PARP3 [R100H](Homo sapiens (Human))
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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
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 tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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
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
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
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
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
Affinity DataIC50: 6nMAssay Description:Inhibition of human recombinant PARP-1 after 1 hr by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 85nMAssay Description:Inhibition of human PARP1More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
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))
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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
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
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
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
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
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
Affinity DataIC50: 4nMAssay Description:Inhibition of human recombinant PARP1 after 1 hr by ELISAMore data for this Ligand-Target Pair
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
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
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
TargetProtein mono-ADP-ribosyltransferase PARP12(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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
TargetProtein mono-ADP-ribosyltransferase PARP12(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetProtein mono-ADP-ribosyltransferase PARP10(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetProtein mono-ADP-ribosyltransferase PARP15(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetProtein mono-ADP-ribosyltransferase PARP10(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetProtein mono-ADP-ribosyltransferase PARP15(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetProtein mono-ADP-ribosyltransferase PARP3(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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 Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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
TargetProtein mono-ADP-ribosyltransferase PARP4(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
TargetProtein mono-ADP-ribosyltransferase PARP4(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
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
TargetProtein mono-ADP-ribosyltransferase PARP3(Homo sapiens (Human))
Health& Science University
Curated by ChEMBL
Health& Science University
Curated by ChEMBL
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
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
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 2(Homo sapiens (Human))
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
US Patent
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