OUL35 [Ligand Id: 13119] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1438938 |
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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 | Inhibition of N-terminal His-tagged human ARTD15 (1 to 280 residues) expressed in Escherichia coli Rosetta2 (DE3) after 24 hrs in presence of NAD+ | B | 5.38 | pIC50 | 4200 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| 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 full length recombinant His6-tagged human PARP1 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of full length recombinant His6-tagged PARP1 catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of N-terminal His-tagged human ARTD1 (1 to 1014 residues) expressed in Escherichia coli Rosetta2 (DE3) using activated DNA as substrate after 1.5 hrs in presence of NAD+ | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of PARP1 (unknown origin) expressed in Escherichia coli Rosette2 (DE3) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2022) 65: 7532-7560 [PMID:35608571] |
| 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 ARTD10 (unknown origin)-induced cell death expressed in human HeLa cells after 10 days by methylene blue staining based colony formation assay | B | 5.87 | pIC50 | 1350 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of PARP10 in human HeLa cells assessed as increase in cell colonies incubated for 10 days with replacement with fresh medium for every 4 days by methylene blue dye based colony formation assay | B | 5.87 | pIC50 | 1350 | nM | IC50 | Eur J Med Chem (2022) 237: 114362-114362 [PMID:35500474] |
| ChEMBL | Inhibition of human PARP10 catalytic domain assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay | B | 5.88 | pIC50 | 1318.26 | nM | IC50 | ACS Med Chem Lett (2019) 10: 74-79 [PMID:30655950] |
| ChEMBL | Inhibition of human PARP10 catalytic domain assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay | B | 5.89 | pIC50 | 1300 | nM | IC50 | ACS Med Chem Lett (2019) 10: 74-79 [PMID:30655950] |
| ChEMBL | Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 6.19 | pIC50 | 645.65 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 6.19 | pIC50 | 640 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) R931A mutant expressed in Escherichia coli Rosetta2 (DE3) Rosetta2 (DE3) using SRPK2 as substrate after 21 hrs in presence of NAD+ | B | 6.22 | pIC50 | 600 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| GtoPdb | - | - | 6.48 | pIC50 | 330 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 13 hrs in presence of NAD+ | B | 6.48 | pIC50 | 330 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of human 6His-tagged PARP10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) cells by fluorescent based analysis | B | 6.48 | pIC50 | 330 | nM | IC50 | Eur J Med Chem (2022) 237: 114362-114362 [PMID:35500474] |
| ChEMBL | Inhibition of PARP10 (unknown origin) expressed in Escherichia coli Rosette2 (DE3) | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2022) 65: 7532-7560 [PMID:35608571] |
| ChEMBL | Inhibition of full length recombinant His6-tagged PARP10 catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | B | 6.48 | pIC50 | 329 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| 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 full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | ACS Med Chem Lett (2019) 10: 74-79 [PMID:30655950] |
| ChEMBL | Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay | B | 5.68 | pIC50 | 2089.3 | nM | IC50 | ACS Med Chem Lett (2019) 10: 74-79 [PMID:30655950] |
| Poly [ADP-ribose] polymerase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429709] [UniProtKB: Q9H0J9] | ||||||||
| ChEMBL | Inhibition of N-terminal His-tagged thioredoxin-fused human ARTD12 (469 to 701 residues) expressed in Escherichia coli Rosetta2 (DE3) after 20 hrs in presence of NAD+ | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| 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 full length recombinant His6-tagged PARP14 catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | B | 4.63 | pIC50 | 23400 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of N-terminal His-tagged thioredoxin-fused human ARTD8 (1535 to 1801 residues) expressed in Escherichia coli Rosetta2 (DE3) after 21 hrs in presence of NAD+ | B | 4.64 | pIC50 | 23000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of PARP14 (unknown origin) | B | 4.64 | pIC50 | 23000 | nM | IC50 | Eur J Med Chem (2022) 237: 114362-114362 [PMID:35500474] |
| ChEMBL | Inhibition of PARP14 (unknown origin) expressed in Escherichia coli Rosette2 (DE3) | B | 4.64 | pIC50 | 23000 | nM | IC50 | J Med Chem (2022) 65: 7532-7560 [PMID:35608571] |
| ChEMBL | Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| 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 N-terminal His-tagged human ARTD7 (482 to 678 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 3 hrs in presence of NAD+ | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of PARP15 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2022) 237: 114362-114362 [PMID:35500474] |
| ChEMBL | Inhibition of PARP15 (unknown origin) expressed in Escherichia coli Rosette2 (DE3) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7532-7560 [PMID:35608571] |
| ChEMBL | Inhibition of full length recombinant His6-tagged PARP15 catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | B | 5.38 | pIC50 | 4170 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| 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 full length recombinant His6-tagged PARP2 catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of N-terminal His-tagged thioredoxin-fused human ARTD2 (1 to 583 residues) expressed in Escherichia coli Rosetta2 (DE3) using activated DNA as substrate after 1.5 hrs in presence of NAD+ | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2022) 237: 114362-114362 [PMID:35500474] |
| ChEMBL | Inhibition of PARP2 (unknown origin) expressed in Escherichia coli Rosette2 (DE3) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2022) 65: 7532-7560 [PMID:35608571] |
| 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 N-terminal His-tagged thioredoxin-fused human ARTD3 (1 to 533 residues) expressed in Escherichia coli Rosetta2 (DE3) using DNA as substrate after 3 hrs in presence of NAD+ | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| Poly [ADP-ribose] polymerase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6142] [UniProtKB: Q9UKK3] | ||||||||
| ChEMBL | Inhibition of N-terminal His-tagged human ARTD4 (250 to 565 residues) expressed in Escherichia coli Rosetta2 (DE3) using TCEP as substrate after 2.5 hrs in presence of NAD+ | B | 4.64 | pIC50 | 23000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271] | ||||||||
| ChEMBL | Inhibition of full length recombinant His6-tagged PARP5A catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of N-terminal His-tagged human ARTD5 (1030 to 1317 residues) expressed in Escherichia coli Rosetta2 (DE3) using TCEP as substrate after 18 hrs in presence of NAD+ | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of TNKS1 (unknown origin) expressed in Escherichia coli Rosette2 (DE3) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2022) 65: 7532-7560 [PMID:35608571] |
| tankyrase 2/Tankyrase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6154] [GtoPdb: 3109] [UniProtKB: Q9H2K2] | ||||||||
| ChEMBL | Inhibition of full length recombinant His6-tagged PARP5B catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2050-2054 [PMID:29748053] |
| ChEMBL | Inhibition of N-terminal His-tagged Z-basic-fused human ARTD6 (873 to 1161 residues) expressed in Escherichia coli Rosetta2 (DE3) using TCEP as substrate after 18 hrs in presence of NAD+ | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2018) 156: 93-102 [PMID:30006177] |
| ChEMBL | Inhibition of TNKS2 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2022) 237: 114362-114362 [PMID:35500474] |
| ChEMBL | Inhibition of TNKS2 (unknown origin) expressed in Escherichia coli Rosette2 (DE3) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2022) 65: 7532-7560 [PMID:35608571] |
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]
