| Assay ID | Title | Year | Journal | Article |
|---|
| AID649227 | Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response. |
| AID748262 | Inhibition of PARP1 (unknown origin) using histone as substrate after 1 hr by luminescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID661315 | Selectivity ratio of IC50 for human PARP2 to IC50 for human TNSK2 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID748257 | Intrinsic clearance in rat liver microsomes | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID525416 | Induction of Axin2 accumulation in human DLD1 cells by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525196 | Effect on Axin2 subcellular redistribution in african green monkey Cos1 cells by immunostaining method | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525202 | Effect on interaction between Axin1-GFP and CK1epsilon in HEK293 cell lysate at 10 uM by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1428387 | 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 | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors. |
| AID722001 | Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket. |
| AID661309 | Selectivity ratio of IC50 for PARP2 to IC50 for TNSK2 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID748253 | Selectivity ratio of IC50 for PARP2 (unknown origin) to IC50 for tankyrase2 (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID748259 | Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID525201 | Effect on interaction between Axin1-GFP and GSK3-beta in HEK293 cell lysate at 10 uM by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525447 | Inhibition of Wnt1/beta-casein pathway activity in mouse L cell expressing Wnt1 and STF assessed as decreased firefly luciferase reporter expression | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID649235 | Cardiogenic activity in human embryonic stem cells at 4 uM by MYH6 reporter gene assay relative to control | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response. |
| AID1156453 | Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID525449 | Induction of Axin1 stabilization in human DLD1 cells overexpressing IWR-IS by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1128299 | Inhibition of TNKS-2 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors. |
| AID722004 | Inhibition of N-terminal His6-tagged human TNKS1 (1091 to 1325 amino acid residues) after 60 mins by autoparsylation assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket. |
| AID525209 | Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Thr41 phosphorylated beta-casein levels by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID649233 | Inhibition of human recombinant TGFbeta2-induced Smad signaling in HEK293T cells at 0.01 to 5 uM by luciferase reporter gene assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response. |
| AID661306 | Inhibition of TNKS2 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID525461 | Induction of Axin2 stabilization in human DLD1 cells assessed as decreased transcription of Axin2 after 2 hrs by RT-PCR method | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1428393 | 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 | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors. |
| AID425207 | Half life in mouse liver S9 fraction | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Structure-activity relationship studies of small-molecule inhibitors of Wnt response. |
| AID661311 | Inhibition of human PARP2 using NAD+ as substrate after 90 mins by fluorescence analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID525210 | Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser37 phosphorylated beta-casein levels by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID661312 | Selectivity ratio of IC50 for human PARP1 to IC50 for human TNSK1 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID525208 | Inhibition of Axin2 protein degradation in human DLD1 cells by Western blot analysis in presence of 100 uM cyclohexamide | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525193 | Displacement of IWR-PB from Axin2 in HEK293 cells by Western blot method | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1866926 | Inhibition of TNKS2 (unknown origin) | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer. |
| AID1428389 | 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 | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors. |
| AID1156480 | Inhibition of Wnt/beta-catenin signaling in zebrafish larvae assessed as inhibition of Tcf/Lef transcriptional activity at 10 uM after 72 hrs by GFP reporter assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID1156456 | Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID425206 | Half life in mouse blood | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Structure-activity relationship studies of small-molecule inhibitors of Wnt response. |
| AID649230 | Cardiogenic activity in human H9 cells after 14 days by MYH6-mCherry reporter gene assay relative to 4-[(1R,2S,6R,7S)-3,5-dioxo-4-azatricyclo[5.2.1.0~2,6~]dec-8-en-4-yl]-N-quinolin-8-ylbenzamide | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response. |
| AID525451 | Inhibition of Wnt3A mediated fgf20a expression in Zebrafish resected tail fins after 24 hrs post amputation | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525454 | Decrease in beta-casein accumulation in human DLD1 cells expressing in APC mutant | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525452 | Inhibition of Wnt3A activity in Zebrafish gastrointestinal tract assessed as decreased BrdU incorporation at 10 uM after 18-14 days | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525441 | Inhibition of Wnt3A/beta-casein pathway activity in mouse L cell expressing Wnt3a assessed as decrease in phosphorylated Dvl2 level at 10 uM after 24 hrs by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1156454 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID525206 | Effect on proteasome in mouse L cell expressing Wnt assessed as accumulation of beta-casein by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID661305 | Inhibition of TNKS1 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID1428394 | 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 | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors. |
| AID525203 | Effect on affinity between Axin2 and beta-casein in HEK293 cell lysate at 10 uM by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID748256 | Selectivity ratio of IC50 for PARP1 (unknown origin) to IC50 for 6XHis-tagged tankyrase1 (1091 to 1325) (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID748261 | Inhibition of PARP2 (unknown origin) using histone as substrate after 1 hr by luminescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID1866925 | Inhibition of TNKS1 (unknown origin) | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer. |
| AID1866927 | Inhibition of PARP1 (unknown origin) | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer. |
| AID525415 | Induction of Axin2 accumulation in human DLD1 cells assessed as decrease in free beta-casein levels by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1754627 | Cytotoxicity against human HT-29 cells assessed as cell viability at 1.563 to 50 uM measured after 72 hrs by plate reader method | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | Linderapyrone: A Wnt signal inhibitor isolated from Lindera umbellata. |
| AID661307 | Activity of N-terminus hexaHis-tagged human TNSK2 expressed in Escherichia coli BL21 (DE3) cells using biotinylated NAD+ as substrate after 90 mins by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID649234 | Cytotoxicity against human HEK293T cells at 0.2 to 20 uM after 24 hrs by alamar blue assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response. |
| AID748260 | Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID748258 | Intrinsic clearance in human liver microsomes | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID661303 | Inhibition of PARP1 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID525442 | Inhibition of Wnt3A/beta-casein pathway activity in mouse L cell expressing Wnt3a assessed as decrease in phosphorylated Lrp6 level at 10 uM after 24 hrs by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1428384 | 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 | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors. |
| AID1128298 | Inhibition of TNKS-1 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors. |
| AID525200 | Effect on interaction between Axin1-GFP and Lrp2 in HEK293 cells transfected with LRP6-myc and Axin2-myc cDNAs at 10 uM by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID722003 | Inhibition of N-terminal His6-tagged human TNKS2 (946 to 1162 amino acid residues) after 60 mins by autoparsylation assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket. |
| AID525446 | Inhibition of Wnt2/beta-casein pathway activity in mouse L cell expressing Wnt2 and STF assessed as decreased firefly luciferase reporter expression | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525197 | Induction of Axin2 stabilization in human DLD1 cells assessed as inhibition of Wnt/beta-casein pathway | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1866928 | Inhibition of PAPR2 (unknown origin) | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer. |
| AID1128314 | Inhibition of tankyrase in human DLD1 cells assessed as inhibition of TCF-dependent transcriptional activity at 1 to 20 uM after 24 hrs by dual luciferase reporter gene assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors. |
| AID525448 | Inhibition of Wnt3A/beta-casein pathway activity in mouse L cell expressing Wnt3A and STF assessed as decreased firefly luciferase reporter expression | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID748254 | Selectivity ratio of IC50 for PARP2 (unknown origin) to IC50 for 6XHis-tagged tankyrase1 (1091 to 1325) (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID722000 | Selectivity ratio of IC50 for N-terminal His6-tagged human TNKS1 (1091 to 1325 amino acid residues) to IC50 for PARP2 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket. |
| AID525462 | Inhibition of Wnt/beta-casein pathway activity in mouse L cell expressing Wnt and STF assessed as decreased firefly luciferase reporter expression | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID748255 | Selectivity ratio of IC50 for PARP1 (unknown origin) to IC50 for tankyrase2 (unknown origin) | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID525204 | Effect on interaction between Axin1-GFP and DVl2 in HEK293 cell lysate at 10 uM by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1156451 | Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID649228 | Chemical stability in phosphate buffer pH 7.4 at 10 uM after 30 hrs by HPLC analysis | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response. |
| AID1156457 | Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control in presence of GSK-3beta inhibitor LiCl | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID1156452 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID425209 | Inhibition of fin regeneration in zebrafish | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Structure-activity relationship studies of small-molecule inhibitors of Wnt response. |
| AID748252 | Half life in mouse plasma at 10 uM after 2 hrs by LC/MS/MS analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID1917763 | Inhibition of Wnt/beta-catenin transactivation signalling in Wnt3a stimulated human HEK293 cells harbouring TCF/LEF luciferase reporter gene assessed as inhibition TCF-beta-catenin complex formation by measuring luminescence level at 50 uM preincubated fo | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Development of a penetratin-conjugated stapled peptide that inhibits Wnt/β-catenin signaling. |
| AID661313 | Selectivity ratio of IC50 for human PARP1 to IC50 for human TNSK2 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID425208 | Half life in mouse hepatocytes | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Structure-activity relationship studies of small-molecule inhibitors of Wnt response. |
| AID1156455 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID525207 | Inhibition of Axin2 protein degradation in human DLD1 cells by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525191 | Induction of Axin2 in human DLD1 cells overexpressing IWR-IS assessed as decrease in Wnt pathway activity at 10 uM by STF reporter assay method | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1156458 | Inhibition of Wnt/beta-catenin signaling in human HT29 cells assessed as increase in axin2 mRNA expression at 25 uM after 24 hrs by quantitative real-time PCR assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling. |
| AID661314 | Selectivity ratio of IC50 for human PARP2 to IC50 for human TNSK1 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID1128315 | Cytotoxicity against human DLD1 cells assessed as growth inhibition at 1 to 20 uM measured on day 10 by crystal violet staining | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors. |
| AID661308 | Selectivity ratio of IC50 for PARP2 to IC50 for TNSK1 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID525440 | Inhibition of Wnt3A/beta-casein pathway activity in mouse L cell expressing Wnt3a assessed as inhibition of beta-casein accumulation at 10 uM after 24 hrs by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525450 | Inhibition of caudal fin regeneration after mechanical resection in zebrafish at 10 uM after 7 days | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID748264 | Inhibition of 6XHis-tagged tankyrase1 (1091 to 1325) (unknown origin) after 60 mins in presence of NAD | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID525198 | Effect on Axin2 subcellular redistribution in human HeLa cells by immunostaining method | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID661304 | Inhibition of PARP2 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID1866923 | Antitumor activity against human MNNG/HOS cells xenografted in mouse assessed as decrease in tumor growth rate at 5 mg/kg, IT administered every other day for 12 days relative to control | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer. |
| AID748263 | Inhibition of tankyrase2 (unknown origin) after 60 mins in presence of NAD | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID722002 | Inhibition of PARP2 (unknown origin) | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket. |
| AID525211 | Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser33 phosphorylated beta-casein levels by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1894736 | Inhibition of Wnt/beta-catenin signaling pathway in mouse L Wnt-3A cells harbouring STF-reporter gene assessed as assessed as reduction in luciferase activity incubated for 24 hrs by luciferase reporter assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling. |
| AID525453 | Decrease in beta-casein accumulation in APC-deficient mouse L cell | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525205 | Effect on proteasome in mouse L cell expressing Wnt assessed as accumulation of Axin1 by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525199 | Effect on interaction between Axin1-GFP and PP2A in HEK293 cell lysate at 10 uM by Western blot analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2
| Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID661310 | Inhibition of human PARP1 using NAD+ as substrate after 90 mins by fluorescence analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Structural basis of selective inhibition of human tankyrases. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2014 | Acta crystallographica. Section D, Biological crystallography, Oct, Volume: 70, Issue:Pt 10
| Insights into the binding of PARP inhibitors to the catalytic domain of human tankyrase-2. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |