NVP‐TNKS656 [Ligand Id: 10674] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2419706
  • poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874]
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  • poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5]
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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) assessed as nicotinamide concentration by LC-MS analysis B 4.72 pIC50 >19000 nM IC50 J. Med. Chem. (2013) 56: 6495-6511 [PMID:23844574]
ChEMBL Biochemical Assay: The autoparsylation activity of the TNKS 1/2 or PARP1/2 enzymes was measured by the liquid chromatography-mass spectrometry (LC/MS) detection of nicotinamide as readout. Compound activity in inhibiting the TNKS and PARP autoparsylation was evaluated by IC50 measurements. In the compound screening assays, the reaction is composed of 5 μL of compound in 8-point serial dilutions with concentrations ranging from 0.0086 to 18.75 μM, 20 nM of purified enzyme, and 250 μM of β-NAD+ in the 1× Assay Buffer. After 60 min incubation at room temperature, the reactions were quenched by the addition of 10 μL of 5× quenching solution (20% formic acid and 500 nM [d]-nicotinamide in water). For the background control wells, 10 μL of the 5× quenching solution per well was added prior to the addition of β-NAD+. B 4.72 pIC50 >19000 nM IC50 US-9181266-B2. 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors (2015)
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) assessed as nicotinamide concentration by LC-MS analysis B 4.49 pIC50 32000 nM IC50 J. Med. Chem. (2013) 56: 6495-6511 [PMID:23844574]
ChEMBL Biochemical Assay: The autoparsylation activity of the TNKS 1/2 or PARP1/2 enzymes was measured by the liquid chromatography-mass spectrometry (LC/MS) detection of nicotinamide as readout. Compound activity in inhibiting the TNKS and PARP autoparsylation was evaluated by IC50 measurements. In the compound screening assays, the reaction is composed of 5 μL of compound in 8-point serial dilutions with concentrations ranging from 0.0086 to 18.75 μM, 20 nM of purified enzyme, and 250 μM of β-NAD+ in the 1× Assay Buffer. After 60 min incubation at room temperature, the reactions were quenched by the addition of 10 μL of 5× quenching solution (20% formic acid and 500 nM [d]-nicotinamide in water). For the background control wells, 10 μL of the 5× quenching solution per well was added prior to the addition of β-NAD+. B 4.72 pIC50 >19000 nM IC50 US-9181266-B2. 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors (2015)
Protein Wnt-3a in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255137] [UniProtKB: P56704]
ChEMBL Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin B 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (2013) 56: 6495-6511 [PMID:23844574]
tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271]
ChEMBL Biochemical Assay: The autoparsylation activity of the TNKS 1/2 or PARP1/2 enzymes was measured by the liquid chromatography-mass spectrometry (LC/MS) detection of nicotinamide as readout. Compound activity in inhibiting the TNKS and PARP autoparsylation was evaluated by IC50 measurements. In the compound screening assays, the reaction is composed of 5 μL of compound in 8-point serial dilutions with concentrations ranging from 0.0086 to 18.75 μM, 20 nM of purified enzyme, and 250 μM of β-NAD+ in the 1× Assay Buffer. After 60 min incubation at room temperature, the reactions were quenched by the addition of 10 μL of 5× quenching solution (20% formic acid and 500 nM [d]-nicotinamide in water). For the background control wells, 10 μL of the 5× quenching solution per well was added prior to the addition of β-NAD+. B 7.81 pIC50 15.5 nM IC50 US-9181266-B2. 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors (2015)
GtoPdb - - 7.81 pIC50 15.5 nM IC50 WO2013012723A1. Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors (2013)
tankyrase 2/Tankyrase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6154] [GtoPdb: 3109] [UniProtKB: Q9H2K2]
GtoPdb - - 8.22 pIC50 6 nM IC50 J Med Chem (2013) 56: 6495-511 [PMID:23844574];
WO2013012723A1. Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors (2013)
ChEMBL Inhibition of TNSK2 (unknown origin) assessed as nicotinamide concentration by LC-MS analysis B 8.22 pIC50 6 nM IC50 J. Med. Chem. (2013) 56: 6495-6511 [PMID:23844574]
ChEMBL Biochemical Assay: The autoparsylation activity of the TNKS 1/2 or PARP1/2 enzymes was measured by the liquid chromatography-mass spectrometry (LC/MS) detection of nicotinamide as readout. Compound activity in inhibiting the TNKS and PARP autoparsylation was evaluated by IC50 measurements. In the compound screening assays, the reaction is composed of 5 μL of compound in 8-point serial dilutions with concentrations ranging from 0.0086 to 18.75 μM, 20 nM of purified enzyme, and 250 μM of β-NAD+ in the 1× Assay Buffer. After 60 min incubation at room temperature, the reactions were quenched by the addition of 10 μL of 5× quenching solution (20% formic acid and 500 nM [d]-nicotinamide in water). For the background control wells, 10 μL of the 5× quenching solution per well was added prior to the addition of β-NAD+. B 8.22 pIC50 6 nM IC50 US-9181266-B2. 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors (2015)

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]