PJ34 [Ligand Id: 11348] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL372303 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 PARP1 by isothermal titration colorimetry | B | 6.96 | pKd | 110 | nM | Kd | J Med Chem (2009) 52: 3108-3111 [PMID:19354255] |
| 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 | 6.32 | pIC50 | 481 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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 | 6.32 | pIC50 | 478.63 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of PARP-1 (unknown origin) assessed as NAD+ consumption after 20 mins by fluorometric analysis in presence of activated DNA | B | 6.77 | pIC50 | 170.2 | nM | IC50 | Bioorg Med Chem (2014) 22: 1700-1707 [PMID:24503274] |
| ChEMBL | Inhibition of PARP1 using TACS-Sapphire substrate for 30 mins by colorimetry | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2012) 50: 264-273 [PMID:22365563] |
| ChEMBL | In vitro inhibitory concentration against Poly(ADP-ribose) polymerase 1 | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4221-4225 [PMID:16098744] |
| ChEMBL | Inhibition of human recombinant PARP1 | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2009) 52: 718-725 [PMID:19125579] |
| ChEMBL | Inhibition of human PARP1 | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2009) 52: 3108-3111 [PMID:19354255] |
| 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 | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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 | 7.22 | pIC50 | 60.26 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of PARP1 | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2010) 53: 4561-4584 [PMID:20364863] |
| ChEMBL | Inhibition of PARP1 in human HeLa cells by fluid scintillation counting using [adenylated-32P]NAD as substrate | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5126-5129 [PMID:18713665] |
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5126-9 [PMID:18713665] |
| 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 | 7.96 | pIC50 | 10.96 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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 | 7.96 | pIC50 | 10.9 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of full length human C-terminal His-tagged PARP1 expressed in baculovirus infected Sf9 cells using chicken core histone as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scintillation counter | B | 8.04 | pIC50 | 9.1 | nM | IC50 | ACS Med Chem Lett (2020) 11: 862-868 [PMID:32435397] |
| ChEMBL | Inhibition of ARTD1 (unknown origin) | B | 7.7 | pEC50 | 20 | nM | EC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| 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 | 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 | 5.17 | pIC50 | 6800 | 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 | 5.17 | pIC50 | 6760.83 | 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 | 5.23 | pIC50 | 5888.44 | 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 | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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 | 6.64 | pIC50 | 230 | 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 | 6.65 | pIC50 | 223.87 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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 recombinant human His6-tagged PARP14 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of recombinant human His6-tagged PARP14 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 5.38 | pIC50 | 4168.69 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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 | 5.05 | pIC50 | 9000 | 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 | 5.05 | pIC50 | 8912.51 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5] | ||||||||
| 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 | 6.42 | pIC50 | 382 | 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 | 6.42 | pIC50 | 380.19 | 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 | 7.47 | pIC50 | 33.5 | 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 | 7.48 | pIC50 | 33.11 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of full length human N-terminal His-tagged PARP2 expressed in baculovirus infected Sf9 cells using histone H3.3 as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scintillation counter | B | 7.83 | pIC50 | 14.7 | nM | IC50 | ACS Med Chem Lett (2020) 11: 862-868 [PMID:32435397] |
| 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 human PARP3 PARP domain by isothermal titration colorimetry | B | 6.15 | pKd | 700 | nM | Kd | J Med Chem (2009) 52: 3108-3111 [PMID:19354255] |
| 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 | 5.84 | pIC50 | 1445.44 | 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 | 5.84 | pIC50 | 1430 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| Poly [ADP-ribose] polymerase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6142] [UniProtKB: Q9UKK3] | ||||||||
| 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 | 6.12 | pIC50 | 758.58 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271] | ||||||||
| 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 | 5.77 | pIC50 | 1698.24 | 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 | 5.77 | pIC50 | 1690 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human 6xhis-tagged ARTD5 (1030 to 1317) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay | B | 5.87 | pIC50 | 1348.96 | nM | IC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| ChEMBL | Inhibition of human 6xhis-tagged ARTD5 (1030 to 1317) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay | B | 5.89 | pIC50 | 1300 | nM | IC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| ChEMBL | Inhibition of 6xhis-tagged ARTD5 (unknown origin) expressed in Escherichia coli BL21 Star (DE3) cells | B | 6.24 | pIC50 | 570 | nM | IC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| ChEMBL | Inhibition of full length human N-terminal GST-tagged TNKS1 ADP-ART catalytic domain (1001 to 1327 residues) using histone H2A as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scintillation counter | B | 7.41 | pIC50 | 39.2 | nM | IC50 | ACS Med Chem Lett (2020) 11: 862-868 [PMID:32435397] |
| tankyrase 2/Tankyrase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6154] [GtoPdb: 3109] [UniProtKB: Q9H2K2] | ||||||||
| 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 | 5.53 | pIC50 | 2951.21 | 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 | 5.54 | pIC50 | 2900 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay | B | 6.66 | pIC50 | 219 | nM | IC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| ChEMBL | Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay | B | 6.66 | pIC50 | 218.78 | nM | IC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| ChEMBL | Inhibition of full length human N-terminal GST-tagged TNKS2 ADP-ART catalytic domain (1001 to 1327 residues) using histone H2A as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scintillation counter | B | 7.28 | pIC50 | 52.7 | nM | IC50 | ACS Med Chem Lett (2020) 11: 862-868 [PMID:32435397] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
