BDBM27566 4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one::Acylpiperazine analogue, 47::Olaparib::US10174023, AZD2281::US10597399, Compound AZD2281::US9187430, AZD-2281::US9255106, AZD2281
SMILES c1ccc2c(c1)C(=NNC2=O)Cc3ccc(c(c3)C(=O)N4CCN(CC4)C(=O)C5CC5)F
InChI Key InChIKey=FDLYAMZZIXQODN-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 222 hits for monomerid = 27566
Affinity DataIC50: 0.100nMAssay Description:Inhibition of PARP-2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.100nMAssay Description:Inhibition of PARP1 (unknown origin) using histone/NAD+ as substrates by NAD/NADH-Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.110nMAssay Description:Inhibition of PARP2 (unknown origin) using histone/NAD+ as substrates by NAD/NADH-Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.130nMAssay Description:Inhibition of N-terminal GST-tagged human PARP2 (2 to 583 residues) expressed in baculovirus-infected Sf9 cells using histone as substrate incubated ...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
Affinity DataKd: 0.270nMAssay Description:Binding affinity to recombinant human PARP-2 by SPR analysisMore data for this Ligand-Target Pair
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: 0.300nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 0.310nMAssay Description:Binding affinity to recombinant human PARP-1 by SPR analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human PARP1 incubated for 90 mins by colorimetric assayMore data for this Ligand-Target Pair
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
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
Affinity DataIC50: 0.411nMAssay Description:Inhibition of C-terminal His-tagged human recombinant PARP-1 (1 to 1014 residues) expressed in Sf9 insect cells incubated for 1 hr by 32P-NAD+-based ...More data for this Ligand-Target Pair
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
Affinity DataIC50: 0.5nMAssay Description:Inhibition of PARP-1 (unknown origin) using Femto-ECL as substrate preincubated for 2.7 hrs followed by substrate addition by chemiluminescence assayMore data for this Ligand-Target Pair
Affinity DataKd: 0.5nMAssay Description:Binding affinity to PARP2 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
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
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
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
Affinity DataIC50: 0.510nMAssay Description:Inhibition of N-terminal GST-tagged full length human PARP1 (2 to 1014 residues) expressed in baculovirus-infected Sf9 cells using histone as substra...More data for this Ligand-Target Pair
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
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
Affinity DataIC50: 0.630nMAssay Description:Inhibition of PARP-1 derived from human HeLa cell nucleusMore data for this Ligand-Target Pair
Affinity DataIC50: 0.730nMAssay Description:Inhibition of PARP-1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 0.800nMAssay Description:Binding affinity to PARP1 (unknown origin) assessed as apparent dissociation constantMore data for this Ligand-Target Pair
Affinity DataIC50: 0.830nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged PARP1 (2 to 1014(end) residues) expressed in Sf9 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 0.870nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583(end) residues) expressed in Sf9 cellsMore data for this Ligand-Target Pair
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
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
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
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
Affinity DataIC50: 1nMAssay Description:Inhibition of PARP-2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
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
Affinity DataIC50: 1nMAssay Description:Inhibition of PARP-2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Binding affinity for estrogen receptor alphaMore data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.10nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Inhibition of recombinant human full-length PARP-2 using biotinylated substrateMore data for this Ligand-Target Pair
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
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
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
Affinity DataIC50: 1.40nMAssay Description:Inhibition of GST-tagged human PARP1 incubated for 30 mins by chemiluminescence based UV/visible spectrophotometric analysisMore data for this Ligand-Target Pair
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
Affinity DataIC50: 1.40nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMAssay Description:Inhibition of GST-tagged human PARP2 incubated for 30 mins by chemiluminescence based UV/visible spectrophotometric analysisMore data for this Ligand-Target Pair

3D Structure (crystal)