rucaparib [Ligand Id: 7736] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1173055 (AG-014699, AG-14447, Rucaparib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Inhibition of recombinant human CDK5/p25 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| DNA polymerase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1828] [UniProtKB: P09884] | ||||||||
| ChEMBL | Inhibition of DNA polymerase alpha (unknown origin) | B | 9.4 | pIC50 | 0.4 | nM | IC50 | RSC Med Chem (2024) 15: 788-808 [PMID:38516587] |
| CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
| ChEMBL | Inhibition of recombinant human CLK1 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761] | ||||||||
| ChEMBL | Inhibition of recombinant human CLK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] | ||||||||
| ChEMBL | Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
| ChEMBL | Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5.63 | pIC50 | 2356 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463] | ||||||||
| ChEMBL | Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5.71 | pIC50 | 1935 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630] | ||||||||
| ChEMBL | Inhibition of recombinant human DYRK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781] | ||||||||
| ChEMBL | Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5.1 | pIC50 | 8030 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20] | ||||||||
| ChEMBL | Inhibition of recombinant human DYRK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of recombinant human GSK-3beta expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| 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 | 5.54 | pKd | 2900 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| 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 PARP1 (unknown origin) assessed as apparent dissociation constant | B | 8.49 | pKd | 3.2 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Inhibition of PARP1 (unknown origin) assessed as inhibition constant | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2021) 64: 2382-2418 [PMID:33650861] |
| GtoPdb | - | - | 8.85 | pKi | 1.4 | nM | Ki | Mol Cancer Ther (2007) 6: 945-56 [PMID:17363489] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4127-4132 [PMID:27353531] |
| ChEMBL | Inhibition of human recombinant full-length PARP1 after 4 mins by [32P]NAD+ incorporation assay | B | 8.85 | pKi | 1.4 | nM | Ki | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
| ChEMBL | Inhibition of human full-length recombinant ARTD1 assessed as incorporation of [32P]NAD+ by scintillation counting analysis | B | 8.85 | pKi | 1.4 | nM | Ki | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| ChEMBL | Binding affinity to PARP1 (unknown origin) assessed as inhibition constant | B | 8.85 | pKi | 1.4 | nM | Ki | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.85 | pKi | 1.4 | nM | Ki | Eur J Med Chem (2020) 203: 112570-112570 [PMID:32717529] |
| 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 | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2020) 28: 115819-115819 [PMID:33120078] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 6.3 | pIC50 | >500 | nM | IC50 | J Med Chem (2015) 58: 3302-3314 [PMID:25761096] |
| 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 | 6.52 | pIC50 | 302 | 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 | 6.52 | pIC50 | 301 | 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 | 7.4 | pIC50 | 39.81 | 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 | 7.4 | pIC50 | 39.8 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of recombinant human GST-tagged PARP1 expressed in Escherichia coli using damaged DNA as substrate after 30 mins in presence of NAD+ by resazurin dye based fluorescence assay | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 847-852 [PMID:29456106] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 7.62 | pIC50 | 23.8 | nM | IC50 | J Med Chem (2022) 65: 16099-16127 [PMID:36512711] |
| ChEMBL | Inhibition of human recombinant PARP1 by ELISA | B | 7.84 | pIC50 | 14.4 | nM | IC50 | Eur J Med Chem (2021) 210: 112954-112954 [PMID:33158576] |
| 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 human recombinant full-length PARP1 after 4 mins by [32P]NAD+ incorporation assay | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2020) 203: 112570-112570 [PMID:32717529] |
| 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 | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.49 | pIC50 | 3.2 | 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 | 8.5 | pIC50 | 3.16 | 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 | 8.7 | pIC50 | 1.98 | nM | IC50 | J Med Chem (2016) 59: 335-357 [PMID:26652717] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9.09 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4557-4561 [PMID:26342868] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2019) 62: 5330-5357 [PMID:31042381] |
| ChEMBL | Inhibition of human PARP1 using NAD+ as substrate incubated for 1 hr by ELISA | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Eur J Med Chem (2022) 227: 113898-113898 [PMID:34656898] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2022) 65: 6803-6825 [PMID:35442700] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| 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 | 9.15 | pIC50 | 0.7 | nM | IC50 | Bioorg Med Chem (2020) 28: 115819-115819 [PMID:33120078] |
| 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 | 7.77 | pEC50 | 17 | 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 | 5.51 | pKd | 3100 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| 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 | 5.64 | pIC50 | 2310 | 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 | 5.64 | pIC50 | 2290.87 | 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 | 6.24 | pIC50 | 570 | 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 | 6.25 | pIC50 | 562.34 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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 | Binding affinity to PARP11 (unknown origin) assessed as apparent dissociation constant | B | 5 | pKd | >10000 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| Poly [ADP-ribose] polymerase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429709] [UniProtKB: Q9H0J9] | ||||||||
| ChEMBL | Binding affinity to PARP12 (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 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 | 5.18 | pIC50 | 6650 | 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 | 5.18 | pIC50 | 6606.93 | 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 | Binding affinity to PARP14 (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 human N-terminal GST/His-tagged recombinant PARP14 (1470 to 1801(end) residues) expressed in Sf9 cells | B | 5.03 | pIC50 | 9300 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| 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 | 5.05 | pIC50 | 8912.51 | 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 | 5.05 | pIC50 | 8830 | 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 | 4.49 | pIC50 | 32600 | 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 | 4.49 | pIC50 | 32359.37 | 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 | Binding affinity to PARP2 (unknown origin) assessed as apparent dissociation constant | B | 7.59 | pKd | 26 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| 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 | 6.76 | pIC50 | 172 | nM | IC50 | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| 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 | 6.86 | pIC50 | 138.04 | 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 | 6.86 | pIC50 | 138 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human recombinant PARP2 by ELISA | B | 7.41 | pIC50 | 38.9 | nM | IC50 | Eur J Med Chem (2021) 210: 112954-112954 [PMID:33158576] |
| 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 | 7.55 | pIC50 | 28.2 | 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 | 7.55 | pIC50 | 28.18 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| ChEMBL | Inhibition of human PARP2 using NAD+ as substrate incubated for 1 hr by ELISA | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Eur J Med Chem (2022) 227: 113898-113898 [PMID:34656898] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2019) 62: 5330-5357 [PMID:31042381] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2022) 65: 6803-6825 [PMID:35442700] |
| 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 | 6.57 | pKd | 267 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| 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 | 6.29 | pIC50 | 512 | 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 | 6.39 | pIC50 | 407.38 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of PARP3 (unknown origin) | B | 7.55 | pIC50 | 28 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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 | 6.3 | pKd | 503 | 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 | 6.08 | pIC50 | 839 | 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 | 6.08 | pIC50 | 831.76 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| 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] |
| Protein mono-ADP-ribosyltransferase PARP9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295895] [UniProtKB: Q8IXQ6] | ||||||||
| ChEMBL | Binding affinity to PARP9 (unknown origin) assessed as apparent dissociation constant | B | 5.51 | pKd | 3100 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271] | ||||||||
| ChEMBL | Binding affinity to PARP5a (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 human recombinant PARP5a (E1023 to T1327 amino acids) incubated for 4 hrs by fluorescence anisotropy binding assay | B | 4.43 | pIC50 | 37000 | nM | IC50 | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Inhibition of recombinant human TNKS1 ADP-ribosyltransferase/sterile alpha motif domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 6.84 | pIC50 | 144.54 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of recombinant human TNKS1 ADP-ribosyltransferase/sterile alpha motif domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 6.84 | pIC50 | 144 | 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 | 7.6 | pIC50 | 25.12 | 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 | 7.6 | pIC50 | 25 | nM | IC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
| 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 | 6.05 | pIC50 | 891.25 | 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 | 6.05 | pIC50 | 890 | 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 | 7.85 | pIC50 | 14.13 | 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 | 7.85 | pIC50 | 14 | nM | IC50 | ACS Med Chem Lett (2014) 5: 18-22 [PMID:24900770] |
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]
