niraparib [Ligand Id: 8275] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1094636 (JNJ-64091742, MK-4827, MK4827, Niraparib, Zejula, ZL-2306) |
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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 | Inhibition of PARP1 (unknown origin) | B | 8.49 | pKi | 3.2 | nM | Ki | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
| 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 | 6.88 | pIC50 | 132 | 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 | 6.88 | pIC50 | 131.83 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human PARP1 catalytic activity after 10 mins by ELISA | B | 7.46 | pIC50 | 35 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4501-4505 [PMID:23850199] |
| ChEMBL | Inhibition of recombinant human GST-fused PARP-1 expressed in Escherichia coli after 30 mins by fluorescence assay | B | 7.49 | pIC50 | 32.3 | nM | IC50 | Bioorg Med Chem (2014) 22: 1089-1103 [PMID:24398383] |
| ChEMBL | Inhibition of GST-tagged recombinant human PARP-1 expressed in Escherichia coli after 30 mins by fluorescence-based assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 462-466 [PMID:24388690] |
| 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 | 7.78 | pIC50 | 16.7 | 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 | 7.79 | pIC50 | 16.22 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human PARP1 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysis | B | 8.09 | pIC50 | 8.05 | nM | IC50 | J Med Chem (2016) 59: 335-357 [PMID:26652717] |
| GtoPdb | - | - | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2009) 52: 7170-85 [PMID:19873981] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4127-4132 [PMID:27353531] |
| ChEMBL | Inhibition of human PARP1 by SPA | B | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2009) 52: 7170-7185 [PMID:19873981] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2015) 58: 3302-3314 [PMID:25761096] |
| ChEMBL | Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay | B | 4.51 | pEC50 | 31000 | 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 | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4501-4505 [PMID:23850199] |
| 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 | 5.48 | pIC50 | 3311.31 | 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 | 5.48 | pIC50 | 3300 | 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 | 5.71 | pIC50 | 1949.84 | 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 | 5.72 | pIC50 | 1900 | 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 | 6.1 | pIC50 | 794.33 | 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 | 7.1 | pIC50 | 79 | 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 | 4.76 | pIC50 | 17300 | 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 | 5.76 | pIC50 | 1737.8 | 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 | 4.53 | pIC50 | 29200 | 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 | 4.54 | pIC50 | 28840.32 | 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 PARP2 (unknown origin) | B | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
| 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 | 7.81 | pIC50 | 15.49 | 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 | 7.82 | pIC50 | 15.3 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human PARP2 by trichloroacetic acid precipitation assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2009) 52: 7170-7185 [PMID:19873981] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
| GtoPdb | - | - | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2009) 52: 7170-85 [PMID:19873981] |
| poly (ADP-ribose) polymerase 3/Poly [ADP-ribose] polymerase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5083] [GtoPdb: 2864] [UniProtKB: Q9Y6F1] | ||||||||
| ChEMBL | Inhibition of human PARP3 by trichloroacetic acid precipitation assay | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (2009) 52: 7170-7185 [PMID:19873981] |
| 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 | 6.53 | pIC50 | 296 | 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 | 6.53 | pIC50 | 295.12 | 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 | 6.35 | pIC50 | 446.68 | 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 | 6.35 | pIC50 | 446 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human v-PARP catalytic domain by trichloroacetic acid precipitation assay | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2009) 52: 7170-7185 [PMID:19873981] |
| 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 | 5.63 | pIC50 | 2355 | 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 | 5.63 | pIC50 | 2344.23 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human TANK1 C-terminal domain by trichloroacetic acid precipitation assay | B | 6.24 | pIC50 | 570 | nM | IC50 | J Med Chem (2009) 52: 7170-7185 [PMID:19873981] |
| 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 | 5.29 | pIC50 | 5130 | 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 | 5.29 | pIC50 | 5128.61 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
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]
