BDBM50446130 AG-014699::AG-14447::RUCAPARIB CAMSYLATE::Rucaparib
SMILES CNCc1ccc(cc1)-c1[nH]c2cc(F)cc3C(=O)NCCc1c23
InChI Key InChIKey=HMABYWSNWIZPAG-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 88 hits for monomerid = 50446130
Affinity DataKi: 0.700nMAssay 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 DataKi: 1.40nMAssay Description:Inhibition of human recombinant full-length PARP1 after 4 mins by [32P]NAD+ incorporation assayMore data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataKi: 1.40nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 1.40nMAssay 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 DataKi: 1.40nMAssay Description:Binding affinity to PARP1 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
Affinity DataKi: 1.40nMAssay Description:Inhibition of human full-length recombinant ARTD1 assessed as incorporation of [32P]NAD+ by scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 2.90nMAssay Description:Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumMore data for this Ligand-Target Pair
Affinity DataIC50: 3.10nMAssay 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
TargetGDH/6PGL endoplasmic bifunctional protein(Homo sapiens (Human))
H. Lee Moffitt Cancer Center & Research Institute
H. Lee Moffitt Cancer Center & Research Institute
Affinity DataIC50: 1.80E+4nMAssay Description:HEK293 H6PD-OE and HEK293 pellets were lysed and the lysate was quantified with the Bradford protein assay. Reaction mix containing galactose-6-phosp...More data for this Ligand-Target Pair
Affinity DataIC50: >500nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.804nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay 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: 4.70nMAssay 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 tankyrase-1(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 145nMAssay Description:Inhibition of recombinant human TNKS1 ADP-ribosyltransferase/sterile alpha motif domain expressed in Escherichia coli BL21(DE3) preincubated for 15 m...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: 832nMAssay 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: 839nMAssay 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 PARP3(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 407nMAssay 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: 138nMAssay 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
TargetPoly [ADP-ribose] polymerase tankyrase-1(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 144nMAssay Description:Inhibition of recombinant human TNKS1 ADP-ribosyltransferase/sterile alpha motif domain expressed in Escherichia coli BL21(DE3) preincubated for 15 m...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: 407nMAssay 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: 3.20nMAssay 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: 138nMAssay 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
Affinity DataIC50: 40nMAssay 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
Affinity DataIC50: 28nMAssay 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
Affinity DataIC50: 302nMAssay 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: 301nMAssay 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: 3.20nMAssay Description:Inhibition of recombinant human His6-tagged PARP1 autophosphorylation at ADP-ribosyltransferase domain by LC-MS/MS methodMore 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: 562nMAssay 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
TargetPoly [ADP-ribose] polymerase tankyrase-2(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 891nMAssay 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 PARP15(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 3.24E+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 PARP15(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 3.26E+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: 2.31E+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
TargetProtein mono-ADP-ribosyltransferase PARP12(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 6.61E+3nMAssay 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 PARP14(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 8.91E+3nMAssay Description:Inhibition of recombinant human His6-tagged PARP14 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: 562nMAssay 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 PARP10(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 570nMAssay 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 PARP12(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 6.65E+3nMAssay 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 PARP14(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 8.83E+3nMAssay Description:Inhibition of recombinant human His6-tagged PARP14 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 tankyrase-2(Homo sapiens (Human))
Health & Science University
Curated by ChEMBL
Health & Science University
Curated by ChEMBL
Affinity DataIC50: 890nMAssay 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
Affinity DataIC50: 26nMAssay Description:Inhibition of recombinant human GST-tagged PARP1 expressed in Escherichia coli using damaged DNA as substrate after 30 mins in presence of NAD+ by re...More data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of PARP2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.800nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.70nMAssay Description:Inhibition of human recombinant full-length PARP1 after 4 mins by [32P]NAD+ incorporation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 17nMAssay 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
Affinity DataIC50: 0.700nMAssay 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: 0.800nMAssay 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: 0.800nMAssay Description:Inhibition of human PARP1 using NAD+ as substrate incubated for 1 hr by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human PARP2 using NAD+ as substrate incubated for 1 hr by ELISAMore data for this Ligand-Target Pair