veliparib [Ligand Id: 7417] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL506871 (ABT-888, PARP-1 INHIBITOR ABT-888, Veliparib) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 | Binding affinity to PARP16 (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 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 | 8.54 | pKd | 2.9 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Binding affinity to recombinant human HisGST-tagged PARP-1 catalytic domain by surface plasmon resonance analysis | B | 8.77 | pKd | 1.7 | nM | Kd | J Med Chem (2015) 58: 6875-6898 [PMID:26222319] |
| ChEMBL | Inhibition of PARP1 (unknown origin) assessed as inhibition constant | B | 8.28 | pKi | 5.2 | nM | Ki | J Med Chem (2021) 64: 2382-2418 [PMID:33650861] |
| ChEMBL | Inhibition of PARP1 (unknown origin) assessed as inhibition constant | B | 8.28 | pKi | 5.2 | nM | Ki | ACS Med Chem Lett (2023) 14: 652-657 [PMID:37197461] |
| ChEMBL | Inhibition of human recombinant PARP1 | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2009) 52: 514-523 [PMID:19143569] |
| ChEMBL | Inhibition of PARP1 by scintillation counting | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2009) 52: 6803-6813 [PMID:19888760] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.48 | pKi | 3.3 | nM | Ki | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| 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 | 6.45 | pIC50 | 354.81 | 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 | 6.45 | pIC50 | 354 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of recombinant human PARP1 expressed in Escherichia coli BL21(DE3) using sheared DNA as substrate measured after 1 hr in presence of NAD+ | B | 6.88 | pIC50 | 132 | nM | IC50 | Eur J Med Chem (2017) 132: 26-41 [PMID:28340412] |
| ChEMBL | Inhibition of recombinant human PARP1 using histone as substrate after 1 hr in presence of NAD+ by ELISA | B | 7.26 | pIC50 | 55 | nM | IC50 | Eur J Med Chem (2018) 145: 389-403 [PMID:29335205] |
| 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 | 7.45 | pIC50 | 35.48 | 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 | 7.45 | pIC50 | 35.2 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1993-1996 [PMID:23481647] |
| ChEMBL | Inhibition of human PARP1 catalytic activity after 10 mins by ELISA | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4501-4505 [PMID:23850199] |
| 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 | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Inhibition of GST-tagged recombinant human PARP-1 expressed in Escherichia coli after 30 mins by fluorescence-based assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 462-466 [PMID:24388690] |
| ChEMBL | Inhibition of PARP-1 (unknown origin) using biotinylated NAD+ as substrate after 60 mins by spectrophotometry | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2014) 57: 5579-5601 [PMID:24922587] |
| ChEMBL | Inhibition of recombinant human GST-fused PARP-1 expressed in Escherichia coli after 30 mins by fluorescence assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem (2014) 22: 1089-1103 [PMID:24398383] |
| ChEMBL | Inhibition of recombinant human PARP1 expressed in Escherichia coli BL21(DE3) using histone as substrate measured after 1 hr in presence of biotinylated NAD+ by ELISA | B | 8.29 | pIC50 | 5.18 | nM | IC50 | Eur J Med Chem (2017) 132: 26-41 [PMID:28340412] |
| ChEMBL | Inhibition of human PARP1 expressed in Escherichia coli using biotinylated histone H1 as substrate measured in presence of [3H]NAD+ by topcount scintillation counting method | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2019) 62: 5330-5357 [PMID:31042381] |
| ChEMBL | Inhibition of PARP-1 (unknown origin) assessed as incorporation of biotinylated poly (ADP-ribose) onto histone protein after 60 mins by TACS-Sapphire substarte-based colorimetric analysis | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2015) 23: 4669-4680 [PMID:26088338] |
| ChEMBL | Inhibition of human PARP1 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysis | B | 8.33 | pIC50 | 4.73 | nM | IC50 | J Med Chem (2016) 59: 335-357 [PMID:26652717] |
| 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 | 8.48 | pIC50 | 3.31 | 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 | 8.48 | pIC50 | 3.3 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.48 | pIC50 | 3.3 | nM | IC50 | ACS Med Chem Lett (2023) 14: 652-657 [PMID:37197461] |
| ChEMBL | Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2019) 62: 5330-5357 [PMID:31042381] |
| ChEMBL | Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay | B | 8.83 | pIC50 | 1.48 | nM | IC50 | J Med Chem (2019) 62: 5330-5357 [PMID:31042381] |
| ChEMBL | Inhibition of PARP-1 (unknown origin) after 1 hr in presence of NAD+/biotinylated NAD+/slDNA by ELISA | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem (2016) 24: 4731-4740 [PMID:27561983] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4127-4132 [PMID:27353531] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 10.21 | pIC50 | 0.06 | nM | IC50 | Eur J Med Chem (2023) 252: 115300-115300 [PMID:36989813] |
| 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 | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4501-4505 [PMID:23850199] |
| 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 | 6.4 | pEC50 | 400 | nM | EC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
| ChEMBL | Inhibition of PARP1 in human C41 cells | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2009) 52: 514-523 [PMID:19143569] |
| ChEMBL | Inhibition of PARP1 in human C41 cells after 30 mins by cell-based assay | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2009) 52: 6803-6813 [PMID:19888760] |
| 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 | 5.17 | pKd | 6800 | 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 | 4.36 | pIC50 | 43800 | 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 | 4.36 | pIC50 | 43651.58 | 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 | 1905.46 | 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 | 4.23 | pIC50 | 59400 | 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 | 4.23 | pIC50 | 58884.37 | 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 | 4.05 | pIC50 | 89125.09 | 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 | 4.05 | pIC50 | 89000 | 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 | 7.96 | pKd | 11 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Binding affinity to recombinant human HisGST-tagged PARP-2 catalytic domain by surface plasmon resonance analysis | B | 8.24 | pKd | 5.8 | nM | Kd | J Med Chem (2015) 58: 6875-6898 [PMID:26222319] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 7.76 | pKi | 17.5 | nM | Ki | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| ChEMBL | Inhibition of human recombinant PARP2 | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2009) 52: 514-523 [PMID:19143569] |
| ChEMBL | Inhibition of PARP2 (unknown origin) assessed as inhibition constant | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2021) 64: 2382-2418 [PMID:33650861] |
| 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 | 6.65 | pIC50 | 225 | 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 | 137 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of recombinant human PARP2 using histone as substrate after 1.5 hr in presence of NAD+ by ELISA | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2018) 145: 389-403 [PMID:29335205] |
| 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 | 7.76 | pIC50 | 17.5 | 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 | 7.76 | pIC50 | 17.38 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
| ChEMBL | Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay | B | 8 | pIC50 | <10 | nM | IC50 | J Med Chem (2019) 62: 5330-5357 [PMID:31042381] |
| ChEMBL | Inhibition of human PARP2 expressed in Escherichia coli using biotinylated histone H1 as substrate measured in presence of [3H]NAD+ by topcount scintillation counting method | B | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2019) 62: 5330-5357 [PMID:31042381] |
| ChEMBL | Inhibition of PARP-2 (unknown origin) after 1 hr in presence of NAD+/biotinylated NAD+/slDNA by ELISA | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem (2016) 24: 4731-4740 [PMID:27561983] |
| 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 | 6.64 | pKd | 231 | 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 | 5.67 | pIC50 | 2137.96 | 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 | 5.69 | pIC50 | 2040 | 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 | Binding affinity to PARP4 (unknown origin) assessed as apparent dissociation constant | B | 6.98 | pKd | 105 | 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 | 5.46 | pIC50 | 3500 | 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 | 5.46 | pIC50 | 3467.37 | 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 | 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 | pIC50 | >100000 | 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 | 4.97 | pIC50 | 10740 | 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 | 4.97 | pIC50 | 10715.19 | 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 | pIC50 | >10000 | 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 | Binding affinity to PARP5b (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 TNKS2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | B | 4.62 | pIC50 | 24000 | 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 | 4.62 | pIC50 | 23988.33 | nM | IC50 | J Med Chem (2017) 60: 1262-1271 [PMID:28001384] |
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]
