AZ6102 [Ligand Id: 11779] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4101890 |
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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 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 | 5.79 | pIC50 | 1621.81 | 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 | 5.8 | pIC50 | 1600 | 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 | 5.47 | pIC50 | 3400 | 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 | 5.57 | pIC50 | 2691.53 | 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 | 4.59 | pIC50 | 25703.96 | 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 | 4.59 | pIC50 | 25600 | 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 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 | 6 | pIC50 | 990 | 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 | 6.01 | pIC50 | 977.24 | 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/sterile alpha motif domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 7 | pIC50 | 100 | 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 | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| GtoPdb | Inhibition of enzymatic activity in vitro | - | 8.22 | pIC50 | 6 | nM | IC50 | ACS Med Chem Lett (2015) 6: 254-9 [PMID:25815142] |
| 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 | 9.22 | pIC50 | 0.6 | 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 | 9.32 | pIC50 | 0.48 | 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]
