olaparib [Ligand Id: 7519] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL521686 (AZ-2281, AZ2281, AZD-2281, AZD2281, KEYLYNK-010 COMPONENT OLAPARIB, KU-0059436, KU-59436, Lynparza, NSC-747856, Olaparib, OLAPARIB COMPONENT OF KEYLYNK-010)
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  • poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874]
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  • poly(ADP-ribose) polymerase family member 10/Poly [ADP-ribose] polymerase 10 in Human [ChEMBL: CHEMBL2429708] [GtoPdb: 3267] [UniProtKB: Q53GL7]
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  • poly(ADP-ribose) polymerase family member 11/Poly [ADP-ribose] polymerase 11 in Human [ChEMBL: CHEMBL2380189] [GtoPdb: 3268] [UniProtKB: Q9NR21]
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  • poly(ADP-ribose) polymerase family member 14/Poly [ADP-ribose] polymerase 14 in Human [ChEMBL: CHEMBL2176777] [GtoPdb: 3269] [UniProtKB: Q460N5]
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  • poly(ADP-ribose) polymerase family member 15/Poly [ADP-ribose] polymerase 15 in Human [ChEMBL: CHEMBL2176778] [GtoPdb: 3270] [UniProtKB: Q460N3]
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  • poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5]
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  • poly (ADP-ribose) polymerase 3/Poly [ADP-ribose] polymerase 3 in Human [ChEMBL: CHEMBL5083] [GtoPdb: 2864] [UniProtKB: Q9Y6F1]
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  • Poly [ADP-ribose] polymerase 4 in Human [ChEMBL: CHEMBL6142] [UniProtKB: Q9UKK3]
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  • TCDD inducible poly(ADP-ribose) polymerase/TCDD-inducible poly [ADP-ribose] polymerase in Human [ChEMBL: CHEMBL2380188] [GtoPdb: 3266] [UniProtKB: Q7Z3E1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Mono [ADP-ribose] polymerase PARP16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105981] [UniProtKB: Q8N5Y8]
ChEMBL Binding affinity to PARP16 (unknown origin) assessed as apparent dissociation constant B 5 pKd >10000 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP16 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.29 pIC50 5128.61 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP16 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.29 pIC50 5100 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874]
ChEMBL Binding affinity to human GST-tagged PARP-1 ART domain (788 to 1014 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant incubated for 30 mins by microscale thermophoresis analysis B 5.27 pKd 5310 nM Kd J Med Chem (2021) 64: 7839-7852 [PMID:34038131]
ChEMBL Binding affinity to PARP1 (unknown origin) assessed as apparent dissociation constant B 9.1 pKd 0.8 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Binding affinity to recombinant human PARP-1 by SPR analysis B 9.51 pKd 0.31 nM Kd J Med Chem (2021) 64: 12089-12108 [PMID:34404206]
ChEMBL Binding affinity to recombinant human HisGST-tagged PARP-1 catalytic domain by surface plasmon resonance analysis B 9.62 pKd 0.24 nM Kd J Med Chem (2015) 58: 6875-6898 [PMID:26222319]
ChEMBL Binding affinity to full length His-tagged PARP1 (unknown origin) after 11 mins in presence of NAD+ by TR-FRET assay B 9.1 pKi 0.79 nM Ki Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL Inhibition of PARP1 (unknown origin) B 5.15 pIC50 7090 nM IC50 J Med Chem (2022) 65: 7016-7043 [PMID:35531606]
ChEMBL Inhibition of PARP1 (unknown origin) incubated for 1 hrs by colorimetric analysis B 5.24 pIC50 5770 nM IC50 RSC Med Chem (2022) 13: 522-567 [PMID:35694689]
ChEMBL Inhibition of human recombinant GST-tagged PARP-1 expressed in Escherichia coli assessed as reduction in NAD+-dependent ADP ribosylation incubated for 30 mins in presence and NAD by resazurin dye based fluorescence analysis B 5.53 pIC50 2960 nM IC50 J Med Chem (2019) 62: 3051-3067 [PMID:30844273]
ChEMBL Inhibition of PARP1 (unknown origin) B 5.9 pIC50 1260 nM IC50 Eur J Med Chem (2022) 230: 114094-114094 [PMID:34998039]
ChEMBL Inhibition of N-terminal GST-tagged human PARP1 expressed in a Baculovirus infected Sf9 insect cells using biotinylated substrate incubated for 1 hr by colorimetric method B 6.86 pIC50 139 nM IC50 Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008]
ChEMBL Inhibition of PARP1 (unknown origin) incubated for 30 mins by fluorescence based analysis B 6.86 pIC50 139 nM IC50 J Med Chem (2022) 65: 16099-16127 [PMID:36512711]
ChEMBL Cellular Assay: Based on the preliminary PARP1 inhibition evaluation of compounds at molecular level by ELISA, compounds were further evaluated for their cellular inhibition against PARP1 using a proliferation inhibition model. B 7.06 pIC50 86.32 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
ChEMBL Inhibition of human PARP1 B 7.07 pIC50 84.96 nM IC50 Bioorg Med Chem Lett (2014) 24: 3739-3743 [PMID:25086680]
ChEMBL Inhibition of recombinant human His6-tagged PARP1 C-3-zinc finger domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 7.16 pIC50 69.18 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL ELISA Assay: The HTb-PARP1 positive clones were obtained using the full-length PARP1 plasmid, through PCR amplification, enzyme digestion, ligation, and transformation into DH5a. The plasmids were extracted and determined by enzyme cleavage, and then transformed into DH10Bac. Bacmid/PARP is determined by PCR and sequencing. TNI was transfected, the viruses were collected, and cells were lysed. PARP1 protein was purified by affinity chromatography and determined by Western blotting. A plate was coated by substrate histone, NAD+ and DNA, as well as expressed PARP1 enzyme, was placed into 96-well plate reaction system. Various reaction conditions were optimized and ultimately determined. B 7.3 pIC50 <50 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
ChEMBL ELISA Assay: The HTb-PARP1 positive clones were obtained using the full-length PARP1 plasmid, through PCR amplification, enzyme digestion, ligation, and transformation into DH5a. The plasmids were extracted and determined by enzyme cleavage, and then transformed into DH10Bac. Bacmid/PARP is determined by PCR and sequencing. TNI was transfected, the viruses were collected, and cells were lysed. PARP1 protein was purified by affinity chromatography and determined by Western blotting. A plate was coated by substrate histone, NAD+ and DNA, as well as expressed PARP1 enzyme, was placed into 96-well plate reaction system. Various reaction conditions were optimized and ultimately determined. B 7.37 pIC50 43 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
ChEMBL Inhibition of recombinant human full length C-terminal His-tagged PARP1 expressed in Sf9 insect cells preincubated for 15 mins followed by NAD+ addition and measured after 40 mins by fluorescence based assay B 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2019) 29: 1904-1908 [PMID:31153806]
ChEMBL Inhibition of PARP1 (unknown origin) by colorimetric assay B 7.47 pIC50 34.15 nM IC50 Eur J Med Chem (2021) 209: 112946-112946 [PMID:33129590]
ChEMBL Inhibition of PARP1 (unknown origin) using Streptavidin-HRP as substrate incubated for 1 hr by absorbance based analysis B 7.47 pIC50 34.15 nM IC50 Eur J Med Chem (2023) 252: 115300-115300 [PMID:36989813]
ChEMBL Inhibition of PARP1 (unknown origin) B 7.69 pIC50 20.3 nM IC50 J Med Chem (2023) 66: 12069-12100 [PMID:37616488]
ChEMBL Inhibition of PARP1 (unknown origin) assessed as reduction in biotinylated poly(ADP-ribose) incorporation on to histone protein by ELISA based colorimetric assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2017) 138: 1135-1146 [PMID:28763648]
ChEMBL Inhibition of PARP1 (unknown origin) by ELISA B 7.72 pIC50 19.1 nM IC50 Eur J Med Chem (2017) 138: 514-531 [PMID:28692916]
ChEMBL Inhibition of recombinant human His6-tagged PARP1 C-3-zinc finger domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 7.72 pIC50 18.9 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP-1 (unknown origin) assessed as incorporation of biotinylated poly ADP-ribose onto histone proteins by colorimetric analysis in presence of GSH and GSTP1 B 7.81 pIC50 15.5 nM IC50 J Med Chem (2014) 57: 2292-2302 [PMID:24521039]
ChEMBL In Vitro Screening Assay: 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 by detecting biotin coupled ADP-ribose that attaches to histone using chemiluminescence method with HT Universal Chemiluminescent PARP Assay Kit With Histone-coated Strip Wells purchased from TREVIGEN. The positive control compound was AZD-2281 purchased from SelleckChem.Method: The kit is based on ELISA. X ul sample/well, Y ul PARP enzyme/well and PARP cocktail 25 ul/well with a total volume of 50 ul/well were added into a 96-well plate coated with histone. Meanwhile, blank control (without enzyme and sample) and negative control (without sample) were set. The plate was incubated at room temperature for 60 min; washed with 1xPBS (+0.1% TritonX-100) for twice; Strep-HRP 50 ul/well was added and incubated at room temperature for 60 min; and then washed with 1xPBS (+0.1% TritonX-100) for twice. B 7.92 pIC50 12 nM IC50 US-9187430-B2. Poly (ADP-ribose) polymerase inhibitor (2015)
ChEMBL Inhibition of PARP1 (unknown origin) incubated for 10 mins using biotinylated NAD+ and activated DNA by colorimetric assay B 7.92 pIC50 11.9 nM IC50 J Med Chem (2015) 58: 8683-8693 [PMID:26469301]
ChEMBL Inhibition of human recombinant PARP1 in presence of NAD+ by ELISA B 7.94 pIC50 11.36 nM IC50 Eur J Med Chem (2022) 240: 114574-114574 [PMID:35785724]
ChEMBL Inhibition of recombinant human PARP1 using histone as substrate after 1 hr in presence of NAD+ by ELISA B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2018) 145: 389-403 [PMID:29335205]
ChEMBL Inhibition of PARP-1 (unknown origin) binding to DNA assessed as DNA trapping activity B 7.97 pIC50 10.62 nM IC50 Bioorg Med Chem Lett (2022) 78: 129046-129046 [PMID:36343904]
ChEMBL Inhibition of recombinant human His6-tagged PARP1 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 7.99 pIC50 10.23 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of GST-tagged recombinant human PARP-1 expressed in Escherichia coli after 30 mins by fluorescence-based assay B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2014) 24: 462-466 [PMID:24388690]
ChEMBL Inhibition of recombinant human His6-tagged PARP1 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 8 pIC50 10 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of human PARP-1 by ELISA B 8.01 pIC50 9.84 nM IC50 Eur J Med Chem (2023) 251: 115243-115243 [PMID:36921527]
ChEMBL Inhibition of human PARP1 expressed in Escherichia coli incubated for 10 mins by colorimetric assay B 8.08 pIC50 8.39 nM IC50 Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008]
ChEMBL Inhibition of recombinant human PARP-1 expressed in Escherichia coli BL21 (DE3) using sheared DNA as substrate in presence of biotinylated NAD after 1 hr by ELISA B 8.09 pIC50 8.1 nM IC50 Bioorg Med Chem (2017) 25: 4045-4054 [PMID:28622906]
ChEMBL Inhibition of PARP1 (unknown origin) by ELISA B 8.09 pIC50 8.06 nM IC50 Eur J Med Chem (2022) 243: 114790-114790 [PMID:36183505]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.1 pIC50 8 nM IC50 J Med Chem (2022) 65: 6803-6825 [PMID:35442700]
ChEMBL Inhibition of PARP-1 (unknown origin) using biotinylated NAD+ as substrate after 60 mins by spectrophotometry B 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5579-5601 [PMID:24922587]
ChEMBL Inhibition of human recombinant N-terminal 6His-6Lys-TEV tagged PARP1 full length expressed in pFastBac expression system incubated for 4 hrs by fluorescence anisotropy binding assay B 8.15 pIC50 7 nM IC50 J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Inhibition of PARP1 (unknown origin) using histone as substrate by ELISA B 8.18 pIC50 6.65 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Binding affinity to PARP1 in human OVCAR8 cells assessed as reduction in [125I]-KX1 binding by gamma counting analysis B 8.22 pIC50 6 nM IC50 J Med Chem (2018) 61: 5367-5379 [PMID:29856625]
ChEMBL Inhibition of PARP1 (unknown origin) by ELISA B 8.22 pIC50 6 nM IC50 RSC Med Chem (2024) 15: 981-997 [PMID:38516606]
ChEMBL Ex vivo inhibition of PARP1 in human SW620 cells assessed as amount of poly(ADP-ribose) by whole cell assay B 8.22 pIC50 6 nM IC50 J Med Chem (2008) 51: 6581-6591 [PMID:18800822]
ChEMBL Inhibition of human recombinant PARP-1 after 1 hr by ELISA B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2014) 24: 2669-2673 [PMID:24815508]
ChEMBL Inhibition of human PARP1 catalytic activity after 10 mins by ELISA B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2013) 23: 4501-4505 [PMID:23850199]
ChEMBL Inhibition of PARP-1 (unknown origin) B 8.28 pIC50 5.22 nM IC50 Bioorg Med Chem Lett (2021) 31: 127710-127710 [PMID:33246105]
ChEMBL Inhibition of recombinant human full-length PARP-1 using biotinylated substrate B 8.29 pIC50 5.1 nM IC50 J Med Chem (2021) 64: 12089-12108 [PMID:34404206]
ChEMBL Inhibition of recombinant human PARP1 using histone as substrate after 1 hr in presence of biotinylated NAD+ by ELISA B 8.3 pIC50 5.01 nM IC50 J Med Chem (2020) 63: 122-139 [PMID:31846325]
GtoPdb Assayed using PARP-1 isolated from HeLa cells, in a scintillation proximity ELISA. - 8.3 pIC50 5 nM IC50 J Med Chem (2008) 51: 6581-91 [PMID:18800822];
J Biomol Screen (2003) 8: 347-52 [PMID:12857389]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2015) 58: 3302-3314 [PMID:25761096]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2016) 26: 4127-4132 [PMID:27353531]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.3 pIC50 5 nM IC50 WO-2018064237-A1. An elisa-like assay for quantifying enzymatic activities of mono-adp-ribosyltransferases (2018)
ChEMBL Inhibition of PARP1 (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2021) 64: 2382-2418 [PMID:33650861]
ChEMBL Inhibition of PARP1 by flashplate scintillation proximity assay B 8.3 pIC50 5 nM IC50 J Med Chem (2008) 51: 6581-6591 [PMID:18800822]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
ChEMBL Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells pre-incubated for 30 mins before addition of activated DNA and NAD by fluorescence based assay B 8.32 pIC50 4.8 nM IC50 J Med Chem (2020) 63: 15541-15563 [PMID:33264017]
ChEMBL Inhibition of recombinant human GST-fused PARP-1 expressed in Escherichia coli after 30 mins by fluorescence assay B 8.35 pIC50 4.5 nM IC50 Bioorg Med Chem (2014) 22: 1089-1103 [PMID:24398383]
ChEMBL Inhibition of PARP1 CD (unknown origin) by colorimetric assay B 8.36 pIC50 4.4 nM IC50 Eur J Med Chem (2023) 252: 115300-115300 [PMID:36989813]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.38 pIC50 4.19 nM IC50 Bioorg Med Chem Lett (2020) 30: 127036-127036 [PMID:32088129]
ChEMBL Inhibition of human recombinant PARP1 after 1 hr by ELISA B 8.4 pIC50 4 nM IC50 J Med Chem (2013) 56: 2885-2903 [PMID:23473053]
ChEMBL Binding affinity to PARP1 (unknown origin) B 8.4 pIC50 3.99 nM IC50 Bioorg Med Chem (2022) 69: 116908-116908 [PMID:35780655]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.4 pIC50 3.99 nM IC50 Eur J Med Chem (2022) 236: 114321-114321 [PMID:35430559]
ChEMBL Inhibition of recombinant full length human N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by UV/Vis spectrophotometric analysis B 8.44 pIC50 3.59 nM IC50 Bioorg Med Chem (2017) 25: 4100-4109 [PMID:28601509]
ChEMBL Inhibition of PARP1 (unknown origin) by colorimetric assay B 8.44 pIC50 3.59 nM IC50 Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008]
ChEMBL Inhibition of human full length PARP1 expressed in Escherichia coli rosetta (DE3) incubated for 20 mins by fluorescence analysis B 8.61 pIC50 2.47 nM IC50 Eur J Med Chem (2021) 209: 112946-112946 [PMID:33129590]
ChEMBL Inhibition of human recombinant PARP1 expressed in Escherichia coli BL21(DE3) incubated for 1 hr by ELISA assay B 8.68 pIC50 2.09 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
ChEMBL Inhibition of recombinant human PARP1 using NAD+ as substrate incubated for 1 hr by ELISA B 8.68 pIC50 2.09 nM IC50 J Med Chem (2021) 64: 16711-16730 [PMID:34748333]
ChEMBL Inhibition of recombinant human PARP1 expressed in Escherichia coli BL21(DE3) using histone as substrate measured after 1 hr in presence of biotinylated NAD+ by ELISA B 8.68 pIC50 2.09 nM IC50 Eur J Med Chem (2017) 132: 26-41 [PMID:28340412]
ChEMBL Inhibition of human PARP1 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysis B 8.71 pIC50 1.94 nM IC50 J Med Chem (2016) 59: 335-357 [PMID:26652717]
ChEMBL Inhibition of recombinant human full length N-terminal GST- tagged PARP1 expressed in baculovirus infected sf9 cells using Colorimetric HRP as substrate incubated for 30 mins by UV/Vis spectrophotometer analysis B 8.74 pIC50 1.8 nM IC50 Eur J Med Chem (2019) 182: 111621-111621 [PMID:31442685]
ChEMBL Inhibition of PARP1 in human T98G cells incubated for 60 mins by immunofluorescence assay B 8.8 pIC50 1.6 nM IC50 J Med Chem (2015) 58: 8683-8693 [PMID:26469301]
ChEMBL Inhibition of PARP1 in human G7 cells incubated for 60 mins by immunofluorescence assay B 8.8 pIC50 1.6 nM IC50 J Med Chem (2015) 58: 8683-8693 [PMID:26469301]
ChEMBL Inhibition of PARP-1 (unknown origin) B 8.81 pIC50 1.55 nM IC50 Eur J Med Chem (2022) 237: 114417-114417 [PMID:35504210]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.83 pIC50 1.49 nM IC50 J Med Chem (2022) 65: 16099-16127 [PMID:36512711]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.85 pIC50 1.4 nM IC50 Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP1 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 8.85 pIC50 1.4 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.85 pIC50 1.4 nM IC50 Eur J Med Chem (2023) 252: 115300-115300 [PMID:36989813]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP1 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 8.86 pIC50 1.38 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP1 (unknown origin) using biotin-NAD+ as substrate incubated for 1 hr by ELISA B 8.9 pIC50 1.26 nM IC50 Eur J Med Chem (2021) 217: 113357-113357 [PMID:33740547]
ChEMBL Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay B 8.92 pIC50 1.2 nM IC50 J Med Chem (2019) 62: 5330-5357 [PMID:31042381]
ChEMBL Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay B 8.93 pIC50 1.18 nM IC50 J Med Chem (2019) 62: 5330-5357 [PMID:31042381]
ChEMBL Inhibition of PARP1 (unknown origin) B 8.96 pIC50 1.1 nM IC50 Bioorg Med Chem Lett (2021) 47: 128169-128169 [PMID:34091044]
ChEMBL Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2015) 25: 5743-5747 [PMID:26546219]
ChEMBL Inhibition of PARP-1 (unknown origin) using biotinylated NAD+ as substrate incubated for 45 mins in the presence of deoxy-oligonucleotide by microplate reader method relative to control B 9 pIC50 1 nM IC50 Eur J Med Chem (2022) 237: 114417-114417 [PMID:35504210]
ChEMBL Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested. B 9.05 pIC50 0.9 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
ChEMBL Inhibition of N-terminal GST-tagged human full length PARP1 (2 to 1041 residues) expressed in baculovirus infected Sf9 cells using histone mixture (H2A and H2B) and biotinylated NAD+ as substrate in presence of activated DNA incubated for 60 mins by chemiluminescence assay B 9.05 pIC50 0.9 nM IC50 Bioorg Med Chem (2020) 28: 115819-115819 [PMID:33120078]
ChEMBL Inhibition of human recombinant N-terminal GST-tagged PARP1 (2 to 1014(end) residues) expressed in Sf9 cells B 9.08 pIC50 0.83 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
ChEMBL Inhibition of PARP-1 (unknown origin) B 9.14 pIC50 0.73 nM IC50 Bioorg Med Chem Lett (2022) 78: 129046-129046 [PMID:36343904]
ChEMBL Inhibition of PARP-1 derived from human HeLa cell nucleus B 9.2 pIC50 0.63 nM IC50 Bioorg Med Chem Lett (2022) 71: 128821-128821 [PMID:35643262]
ChEMBL Inhibition of PARP1 (unknown origin) incubated for 45 mins in presence of biotinylated-NAD+ by microplate reader analysis B 9.22 pIC50 0.6 nM IC50 J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL Inhibition of PARP1 (unknown origin) using biotinylated NAD+ as substrate by microplate reader method B 9.22 pIC50 0.6 nM IC50 Eur J Med Chem (2022) 230: 114116-114116 [PMID:35091172]
ChEMBL Inhibition of N-terminal GST-tagged full length human PARP1 (2 to 1014 residues) expressed in baculovirus-infected Sf9 cells using histone as substrate incubated for 60 mins in presence of activated DNA, NAD+, NAD+-biotin by luminescence based analysis B 9.29 pIC50 0.51 nM IC50 J Med Chem (2023) 66: 13768-13787 [PMID:37752013]
ChEMBL 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 filter binding assay B 9.39 pIC50 0.41 nM IC50 RSC Med Chem (2023) 14: 1309-1330 [PMID:37484567]
ChEMBL Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay B 4.8 pEC50 16000 nM EC50 Bioorg Med Chem Lett (2013) 23: 4501-4505 [PMID:23850199]
ChEMBL 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 temozolomide B 7.22 pEC50 60 nM EC50 Bioorg Med Chem Lett (2013) 23: 4501-4505 [PMID:23850199]
ChEMBL Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 0.5 hrs by fluorescence polarization assay based DNA trapping activity assay B 7.8 pEC50 16 nM EC50 J Med Chem (2020) 63: 15541-15563 [PMID:33264017]
ChEMBL Inhibition of PARP-1 in human HeLa cells assessed as decrease of H2O2-induced PARylation after 3 hrs by fluorescence assay B 8.6 pEC50 2.5 nM EC50 Bioorg Med Chem (2014) 22: 1089-1103 [PMID:24398383]
ChEMBL Inhibition of PARP-1 in human HeLa cells incubated for 18 hrs in presence of H2O2 B 9.4 pEC50 0.4 nM EC50 J Med Chem (2020) 63: 15541-15563 [PMID:33264017]
poly(ADP-ribose) polymerase family member 10/Poly [ADP-ribose] polymerase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429708] [GtoPdb: 3267] [UniProtKB: Q53GL7]
ChEMBL Binding affinity to PARP10 (unknown origin) assessed as apparent dissociation constant B 5.01 pKd 9700 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.03 pIC50 9332.54 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.03 pIC50 9300 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human His6-tagged PARP10 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.9 pIC50 1258.93 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human His6-tagged PARP10 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.9 pIC50 1250 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP10 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 5.97 pIC50 1063.6 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of human N-terminal FLAG-tagged/C-terminal Strep-tagged recombinant PARP10 (805 to 1025 residues) expressed in Sf9 cells B 6.46 pIC50 350 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
poly(ADP-ribose) polymerase family member 11/Poly [ADP-ribose] polymerase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2380189] [GtoPdb: 3268] [UniProtKB: Q9NR21]
ChEMBL Inhibition of PARP11 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 5.11 pIC50 7811 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
Poly [ADP-ribose] polymerase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429709] [UniProtKB: Q9H0J9]
ChEMBL Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 4.99 pIC50 10232.93 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5 pIC50 10050 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP12 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 5.93 pIC50 1162.6 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of human N-terminal FLAG/His-tagged recombinant PARP12 (500 to 701(end) residues) expressed in Sf9 cells B 6.16 pIC50 690 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
poly(ADP-ribose) polymerase family member 14/Poly [ADP-ribose] polymerase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176777] [GtoPdb: 3269] [UniProtKB: Q460N5]
ChEMBL Inhibition of PARP14 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 4.81 pIC50 15563 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
poly(ADP-ribose) polymerase family member 15/Poly [ADP-ribose] polymerase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176778] [GtoPdb: 3270] [UniProtKB: Q460N3]
ChEMBL Inhibition of recombinant human His6-tagged PARP15 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 4.75 pIC50 17782.79 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human His6-tagged PARP15 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 4.75 pIC50 17600 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP15 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 4.84 pIC50 14601 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of N-terminal His-tagged human PARP15 catalytic domain (481 to 678 residues) expressed in Escherichia coli BL21 (DE3) cells up to 100 uM in presence of NAD+ incubated for 2 hrs by M-ELISA plate method B 5.1 pIC50 7943.28 nM IC50 WO-2018064237-A1. An elisa-like assay for quantifying enzymatic activities of mono-adp-ribosyltransferases (2018)
ChEMBL Inhibition of N-terminal His-tagged human PARP15 catalytic domain (481 to 678 residues) expressed in Escherichia coli BL21 (DE3) cells up to 100 uM in presence of NAD+ incubated for 2 hrs by M-ELISA plate method B 5.14 pIC50 7300 nM IC50 WO-2018064237-A1. An elisa-like assay for quantifying enzymatic activities of mono-adp-ribosyltransferases (2018)
ChEMBL Inhibition of human N-terminal GST-tagged recombinant PARP15 (221 to 444(end) residues) expressed in Escherichia coli B 5.59 pIC50 2600 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5]
ChEMBL Binding affinity to PARP2 (unknown origin) assessed as apparent dissociation constant B 9.3 pKd 0.5 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Binding affinity to recombinant human HisGST-tagged PARP-2 catalytic domain by surface plasmon resonance analysis B 9.55 pKd 0.28 nM Kd J Med Chem (2015) 58: 6875-6898 [PMID:26222319]
ChEMBL Binding affinity to recombinant human PARP-2 by SPR analysis B 9.57 pKd 0.27 nM Kd J Med Chem (2021) 64: 12089-12108 [PMID:34404206]
ChEMBL Inhibition of recombinant human His6-tagged PARP2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 6.6 pIC50 251.19 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human His6-tagged PARP2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 6.6 pIC50 251 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP2 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 7.91 pIC50 12.3 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP2 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 7.91 pIC50 12.3 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of human PARP-2 by ELISA B 8.12 pIC50 7.64 nM IC50 Eur J Med Chem (2023) 251: 115243-115243 [PMID:36921527]
ChEMBL Inhibition of human recombinant N-terminal Avi-6His-TEV tagged PARP2 full length expressed in pFastBac expression system incubated for 4 hrs by fluorescence anisotropy binding assay B 8.22 pIC50 6 nM IC50 J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Inhibition of recombinant human PARP2 using histone as substrate after 1.5 hr in presence of NAD+ by ELISA B 8.52 pIC50 3 nM IC50 Eur J Med Chem (2018) 145: 389-403 [PMID:29335205]
ChEMBL Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2015) 25: 5743-5747 [PMID:26546219]
ChEMBL Inhibition of PARP-2 (unknown origin) binding to DNA assessed as DNA trapping activity B 8.53 pIC50 2.93 nM IC50 Bioorg Med Chem Lett (2022) 78: 129046-129046 [PMID:36343904]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by UV/Vis spectrophotometric analysis B 8.55 pIC50 2.81 nM IC50 Bioorg Med Chem (2017) 25: 4100-4109 [PMID:28601509]
ChEMBL Inhibition of PARP2 (unknown origin) B 8.55 pIC50 2.81 nM IC50 Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008]
ChEMBL Inhibition of recombinant human PARP2 using NAD+ as substrate incubated for 1 hr by ELISA B 8.65 pIC50 2.26 nM IC50 J Med Chem (2021) 64: 16711-16730 [PMID:34748333]
ChEMBL Inhibition of human recombinant PARP2 expressed in Escherichia coli BL21(DE3) incubated for 1 hr by ELISA assay B 8.69 pIC50 2.05 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
ChEMBL Inhibition of PARP-2 (unknown origin) B 8.73 pIC50 1.87 nM IC50 Bioorg Med Chem Lett (2021) 31: 127710-127710 [PMID:33246105]
ChEMBL Inhibition of recombinant human PARP-2 expressed in Escherichia coli BL21 (DE3) using sheared DNA as substrate in presence of biotinylated NAD after 1 hr by ELISA B 8.77 pIC50 1.7 nM IC50 Bioorg Med Chem (2017) 25: 4045-4054 [PMID:28622906]
ChEMBL Inhibition of PARP2 (unknown origin) using histone as substrate by ELISA B 8.77 pIC50 1.68 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of recombinant human full-length PARP-2 using biotinylated substrate B 8.92 pIC50 1.2 nM IC50 J Med Chem (2021) 64: 12089-12108 [PMID:34404206]
ChEMBL Inhibition of PARP2 (unknown origin) B 9 pIC50 1.01 nM IC50 Eur J Med Chem (2022) 236: 114321-114321 [PMID:35430559]
GtoPdb Assayed using PARP-2 isolated from HeLa cells, in a scintillation proximity ELISA. - 9 pIC50 1 nM IC50 J Med Chem (2008) 51: 6581-91 [PMID:18800822];
J Biomol Screen (2003) 8: 347-52 [PMID:12857389]
ChEMBL Inhibition of PARP2 (unknown origin) B 9 pIC50 1 nM IC50 J Med Chem (2021) 64: 2382-2418 [PMID:33650861]
ChEMBL Inhibition of recombinant PARP2 by flashplate scintillation proximity assay B 9 pIC50 1 nM IC50 J Med Chem (2008) 51: 6581-6591 [PMID:18800822]
ChEMBL Inhibition of PARP2 (unknown origin) B 9 pIC50 1 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
ChEMBL Inhibition of recombinant human PARP2 using histone as substrate after 1 hr in presence of biotinylated NAD+ by ELISA B 9 pIC50 1 nM IC50 J Med Chem (2020) 63: 122-139 [PMID:31846325]
ChEMBL Inhibition of PARP2 (unknown origin) B 9 pIC50 1 nM IC50 Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747]
ChEMBL Inhibition of PARP2 (unknown origin) B 9 pIC50 1 nM IC50 Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]
ChEMBL Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583(end) residues) expressed in Sf9 cells B 9.06 pIC50 0.87 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
ChEMBL Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay B 9.3 pIC50 0.5 nM IC50 J Med Chem (2019) 62: 5330-5357 [PMID:31042381]
ChEMBL Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested. B 9.35 pIC50 0.45 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
ChEMBL Inhibition of PARP-2 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay B 9.4 pIC50 0.4 nM IC50 J Med Chem (2020) 63: 15541-15563 [PMID:33264017]
ChEMBL Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay B 9.4 pIC50 0.4 nM IC50 J Med Chem (2019) 62: 5330-5357 [PMID:31042381]
ChEMBL Inhibition of N-terminal GST-tagged human PARP2 (2 to 583 residues) expressed in baculovirus-infected Sf9 cells using histone as substrate incubated for 60 mins in presence of activated DNA, NAD+, NAD+-biotin by luminescence based analysis B 9.89 pIC50 0.13 nM IC50 J Med Chem (2023) 66: 13768-13787 [PMID:37752013]
ChEMBL Inhibition of PARP-2 (unknown origin) B 10 pIC50 0.1 nM IC50 Bioorg Med Chem Lett (2022) 78: 129046-129046 [PMID:36343904]
poly (ADP-ribose) polymerase 3/Poly [ADP-ribose] polymerase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5083] [GtoPdb: 2864] [UniProtKB: Q9Y6F1]
ChEMBL Binding affinity to PARP3 (unknown origin) assessed as apparent dissociation constant B 8.24 pKd 5.8 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
GtoPdb - - 8.24 pKd 5.8 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested. B 6.49 pIC50 320 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
ChEMBL Inhibition of full length recombinant human His6-tagged PARP3 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 6.64 pIC50 230 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of full length recombinant human His6-tagged PARP3 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 6.64 pIC50 229.09 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP3 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 7.26 pIC50 55.4 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of PARP3 (unknown origin) using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 7.34 pIC50 46 nM IC50 Bioorg Med Chem Lett (2015) 25: 5743-5747 [PMID:26546219]
ChEMBL Inhibition of human recombinant N-terminal GST-tagged PARP3 (2 to 540(end) residues) expressed in Sf9 cells B 7.41 pIC50 39 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
Poly [ADP-ribose] polymerase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6142] [UniProtKB: Q9UKK3]
ChEMBL Binding affinity to PARP4 (unknown origin) assessed as apparent dissociation constant B 6.85 pKd 141 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Inhibition of recombinant human His6-tagged PARP4 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 6.39 pIC50 410 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human His6-tagged PARP4 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 6.39 pIC50 407.38 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of PARP4 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 7.87 pIC50 13.5 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
Poly [ADP-ribose] polymerase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2380187] [UniProtKB: Q2NL67]
ChEMBL Inhibition of PARP6 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 5.46 pIC50 3479.5 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 5.74 pIC50 1800 nM IC50 Bioorg Med Chem Lett (2015) 25: 5743-5747 [PMID:26546219]
ChEMBL Inhibition of human recombinant N-terminal GST-tagged PARP6 (1 to 630(end) residues) expressed in Sf9 cells B 6.92 pIC50 120 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
Poly [ADP-ribose] polymerase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091262] [UniProtKB: Q8N3A8]
ChEMBL Binding affinity to PARP8 (unknown origin) assessed as apparent dissociation constant B 5 pKd >10000 nM Kd J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Inhibition of PARP8 (unknown origin) B 6.62 pIC50 240 nM IC50 J Med Chem (2023) 66: 14095-14115 [PMID:37843892]
tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271]
ChEMBL Inhibition of human recombinant PARP5a (E1023 to T1327 amino acids) incubated for 4 hrs by fluorescence anisotropy binding assay B 4.15 pIC50 >70000 nM IC50 J Med Chem (2021) 64: 14498-14512 [PMID:34570508]
ChEMBL Inhibition of human recombinant TNKS in DLD1-Wnt-Luc cells after 20 to 22 hrs by luciferase reporter assay B 5.45 pIC50 3534 nM IC50 Medchemcomm (2015) 6: 1687-1692
ChEMBL Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 5.72 pIC50 1900 nM IC50 Bioorg Med Chem Lett (2015) 25: 5743-5747 [PMID:26546219]
ChEMBL Inhibition of PARP5A (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 5.74 pIC50 1816.5 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected sf9 cells using histone as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 5.74 pIC50 1800 nM IC50 J Med Chem (2018) 61: 5367-5379 [PMID:29856625]
ChEMBL Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested. B 5.77 pIC50 1700 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
ChEMBL Inhibition of TNKS1 (unknown origin) using biotin-NAD+ as substrate incubated for 1 hr in the presence of deoxy-oligonucleotide by ELISA analysis relative to control B 5.8 pIC50 1568 nM IC50 Eur J Med Chem (2022) 237: 114417-114417 [PMID:35504210]
ChEMBL Inhibition of histidine-tagged recombinant tankyrase-1 by flashplate scintillation proximity assay B 5.82 pIC50 1500 nM IC50 J Med Chem (2008) 51: 6581-6591 [PMID:18800822]
ChEMBL Inhibition of recombinant human TNKS1 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.91 pIC50 1230.27 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human TNKS1 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.91 pIC50 1230 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested. B 7.98 pIC50 10.4 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
tankyrase 2/Tankyrase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6154] [GtoPdb: 3109] [UniProtKB: Q9H2K2]
ChEMBL Inhibition of PARP5B (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 5.32 pIC50 4775 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]
ChEMBL Inhibition of TNKS2 (unknown origin) using biotin-NAD+ as substrate incubated for 1 hr in the presence of deoxy-oligonucleotide by ELISA analysis relative to control B 5.39 pIC50 4090.5 nM IC50 Eur J Med Chem (2022) 237: 114417-114417 [PMID:35504210]
ChEMBL Inhibition of recombinant human TNKS2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.63 pIC50 2344.23 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of recombinant human TNKS2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay B 5.63 pIC50 2340 nM IC50 J Med Chem (2017) 60: 1262-1271 [PMID:28001384]
ChEMBL Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 5.77 pIC50 1700 nM IC50 Bioorg Med Chem Lett (2015) 25: 5743-5747 [PMID:26546219]
ChEMBL Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected sf9 cells using histone as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay B 5.92 pIC50 1200 nM IC50 J Med Chem (2018) 61: 5367-5379 [PMID:29856625]
ChEMBL Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested. B 8.28 pIC50 5.2 nM IC50 US-9255106-B2. Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors (2016)
TCDD inducible poly(ADP-ribose) polymerase/TCDD-inducible poly [ADP-ribose] polymerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2380188] [GtoPdb: 3266] [UniProtKB: Q7Z3E1]
ChEMBL Inhibition of PARP7 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay B 5.33 pIC50 4700 nM IC50 J Med Chem (2023) 66: 12284-12303 [PMID:37605459]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]