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

Data  171 IC50  13 Kd  6 EC50

PDB links: 8 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 190 hits for monomerid = 27566   

TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 6nMAssay Description:Inhibition of human PARP1 catalytic activity after 10 mins by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
3/9/2009
Entry Details Article
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 tankyrase-1(Human)
Kudos Pharmaceuticals

LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 1.50E+3nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/9/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
9/6/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
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)
TargetProtein mono-ADP-ribosyltransferase PARP3 [R100H](Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent

TargetPoly [ADP-ribose] polymerase tankyrase-1(Human)
Kudos Pharmaceuticals

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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase tankyrase-1(Human)
Kudos Pharmaceuticals

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
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
1/27/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
2/7/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
2/11/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 6nMAssay Description:Inhibition of human recombinant PARP-1 after 1 hr by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 85nMAssay Description:Inhibition of human PARP1More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 5nMAssay Description:Inhibition of PARP1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/4/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
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 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
6/13/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
6/13/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human recombinant PARP1 after 1 hr by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/16/2019
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase tankyrase-1(Human)
Kudos Pharmaceuticals

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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein mono-ADP-ribosyltransferase PARP12(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetPoly [ADP-ribose] polymerase 2(Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
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)
TargetProtein mono-ADP-ribosyltransferase PARP12(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetProtein mono-ADP-ribosyltransferase PARP10(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetProtein mono-ADP-ribosyltransferase PARP15(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetProtein mono-ADP-ribosyltransferase PARP10(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetProtein mono-ADP-ribosyltransferase PARP15(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetProtein mono-ADP-ribosyltransferase PARP3(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein mono-ADP-ribosyltransferase PARP4(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetProtein mono-ADP-ribosyltransferase PARP4(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein mono-ADP-ribosyltransferase PARP3(Human)
Health & Science University

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMed
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 1(Human)
Takeda California

Curated by ChEMBL
LigandPNGBDBM27566(4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbo...)
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
In Depth
Date in BDB:
5/12/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPoly [ADP-ribose] polymerase 2(Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences

US Patent
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)
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