Compile Data Set for Download or QSAR
Report error Found 35 Enz. Inhib. hit(s) for PDB: 8HLJ
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
2/17/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
2/17/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Mouse)
Kudos Pharmaceuticals

LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
In Depth
Date in BDB:
3/9/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of PARP2 (unknown origin) using histone as substrate by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
3/3/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 2.10nMAssay Description:Inhibition of human recombinant PARP2 expressed in Escherichia coli BL21(DE3) incubated for 1 hr by ELISA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
3/2/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 7.60nMAssay Description:Inhibition of human PARP-2 by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Nerviano Medical Sciences

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
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)