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Report error Found 16 Enz. Inhib. hit(s) for PDB: 3U9Y
TargetPoly [ADP-ribose] polymerase tankyrase-2(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 tankyrase-1(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 tankyrase-2(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(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(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(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(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(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(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(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
TargetPoly [ADP-ribose] polymerase tankyrase-1(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(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(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
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 tankyrase-2(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
TargetPoly [ADP-ribose] polymerase tankyrase-1(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