| Assay ID | Title | Year | Journal | Article |
|---|
| AID1142721 | Cytotoxicity against CHO cells assessed as endoreduplicated cells in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142746 | Toxicity in po dosed dog administered qd for 4 weeks measured after 2 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1733255 | Inhibition of recombinant human GST-fused ALK5 expressed in baculovirus infected Sf9 cells assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors. |
| AID1563851 | Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| AID1139885 | Drug metabolism in po dosed rat urine assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-ol by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1256662 | Inhibition of ALK5 in human HaCaT cells assessed as residual enzyme activity at 100 nM by p3TP-luciferase assay relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142714 | Mutagenic activity in Salmonella typhimurium TA1535 at 50 to 5000 ug/plate in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142735 | Toxicity in po dosed female rat administered qd for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142715 | Mutagenic activity in Salmonella typhimurium TA1537 at 50 to 5000 ug/plate in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142742 | Toxicity in dog assessed as effect on hematology at 3 to 30 mg/kg/day, po qd administered for 4 weeks measured after 2 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142614 | Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142615 | Inhibition of ALK4 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142632 | Inhibition of wild-type PDGFR-alpha (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142592 | Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142611 | Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142690 | Cardiotoxicity in po dosed beagle dog assessed as effect on ECG | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142731 | Toxicity in female rat assessed as extramedullary hematopoiesis in spleen at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142620 | Inhibition of MAP4K4 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142646 | Inhibition of VEGFR1 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142736 | AUC (0 to 6 hrs) in male rat at 50 mg/kg/day, po qd after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142633 | Inhibition of wild-type PDGFR-alpha (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139875 | Drug metabolism in po dosed rat bile assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazole-2-carboxylic acid by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142694 | Toxicity in Sprague-Dawley rat assessed as decreased activity at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142652 | Inhibition of VEGFR3 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142594 | Selectivity index, ratio of IC50 for human recombinant p38alpha to IC50 for human recombinant ALK5 | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139888 | Drug metabolism in po dosed rat feces assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazole-2-carbaldehyde by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142727 | Toxicity in male rat assessed as growth plate thickening in sternum at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142712 | Mutagenic activity in Salmonella typhimurium TA98 at 50 to 5000 ug/plate in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142750 | Toxicity in Sprague-Dawley rat assessed as salivation at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142647 | Inhibition of VEGFR2 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142618 | Inhibition of ALK4 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142745 | Toxicity in dog assessed as microscopic observation at 3 to 30 mg/kg/day, po qd administered for 4 weeks measured after 2 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139873 | Drug metabolism in po dosed rat urine assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazole-2-carboxylic acid by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142682 | Inhibition of human ERG channel expressed in HEK293 cells at 10 uM after 3 to 5.7 mins by whole-cell patch clamp technique | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139877 | Drug metabolism in po dosed rat plasma assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazole-2-carboxylic acid by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1139874 | Retention time of the compound in po dosed rat plasma by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142713 | Mutagenic activity in Salmonella typhimurium TA100 at 50 to 5000 ug/plate in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142741 | Toxicity in dog assessed as effect on ECG at 3 to 30 mg/kg/day, po qd administered for 4 weeks measured after 2 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142638 | Inhibition of RIPK2 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142698 | Toxicity in Sprague-Dawley rat assessed as decrease in respiratory rate at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142739 | Cmax in female rat at 50 mg/kg/day, po qd after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142634 | Inhibition of wild-type PDGFR-alpha (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142666 | Antitumor activity against mouse B16 cells in mouse assessed as suppression of tumor volume at 2.5 mg/kg, po qd relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1634304 | Selectivity index, ratio of IC50 for human recombinant untagged p38aplha to IC50 for human recombinant GST-tagged ALK5 | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
| Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| AID1142626 | Inhibition of MINK1 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142653 | Inhibition of VEGFR3 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142686 | Inhibition of human ERG channel expressed in HEK293 cells after 3 to 5.7 mins by whole-cell patch clamp technique | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142747 | AUC (0 to 6 hrs) in dog at 30 mg/kg/day, po qd measured on day 28 | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142655 | Selectivity index, ratio of IC50 for ALK4 (unknown origin) to IC50 for ALK5 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142606 | Inhibition of ALK1 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142729 | Toxicity in female rat assessed as panlobular hypertrophy in liver at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142697 | Toxicity in Sprague-Dawley rat assessed as lacrimation at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142696 | Toxicity in Sprague-Dawley rat assessed as difficulty in breathing at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142683 | Inhibition of human ERG channel expressed in HEK293 cells at 30 uM after 3 to 5.7 mins by whole-cell patch clamp technique | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142674 | Inhibition of CYP2C9 in human liver microsomes using tolbutamide as substrate at 10 uM incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142662 | Competitive inhibition of ALK5 (unknown origin) assessed as increase in apparent Km for ATP at 1 to 370 nM by Michaelis-Menten plot analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142706 | Toxicity in po dosed Sprague-Dawley rat assessed as reduction in activity | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142660 | Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142709 | Mutagenic activity in Salmonella typhimurium TA1535 at 50 to 5000 ug/plate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142622 | Inhibition of MAP4K4 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142711 | Mutagenic activity in Escherichia coli WP2 uvrA at 50 to 5000 ug/plate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139876 | Drug metabolism in po dosed rat feces assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazole-2-carboxylic acid by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142631 | Inhibition of wild-type PDGFR-alpha (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142664 | Competitive inhibition of ALK5 (unknown origin) assessed as enzyme/ATP complex by Michaelis-Menten plot analysis in presence of ATP | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142665 | Antitumor activity against mouse B16 cells in mouse assessed as inhibition of tumor growth at 2.5 mg/kg, po qd relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142651 | Inhibition of VEGFR3 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142612 | Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142625 | Inhibition of MINK1 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139886 | Drug metabolism in po dosed rat plasma assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazole-2-carbaldehyde by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142705 | Toxicity in Sprague-Dawley rat assessed as effect on respiratory parameter at 10 to 100 mg/kg, po | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142595 | Inhibition of ALK5 in human HaCaT cells assessed as residual activity at 0.03 uM after 24 hrs by luciferase reporter gene assay relative to control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142724 | Toxicity in male rat assessed as tubular hypertrophy in kidney at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142616 | Inhibition of ALK4 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142701 | Mutagenic activity in Salmonella typhimurium TA98 at 50 to 5000 ug/plate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142641 | Inhibition of TGFbetaR2 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142609 | Inhibition of ALK4 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142667 | Antitumor activity against mouse B16 cells in mouse assessed as inhibition of lymph node metastasis at 2.5 mg/kg, po qd relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142593 | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142710 | Mutagenic activity in Salmonella typhimurium TA1537 at 50 to 5000 ug/plate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142637 | Inhibition of RIPK2 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142613 | Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142630 | Inhibition of PDGFR-alpha V561D mutant (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142695 | Toxicity in Sprague-Dawley rat assessed as low carriage at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142730 | Toxicity in female rat assessed as tubular hypertrophy in kidney at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142679 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139887 | Drug metabolism in po dosed rat bile assessed as formation of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazole-2-carbaldehyde by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142654 | Inhibition of VEGFR3 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142675 | Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142649 | Inhibition of VEGFR2 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142738 | AUC (0 to 6 hrs) in female rat at 50 mg/kg/day, po qd after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142596 | Solubility of the compound in aqueous buffer at pH 1.2 after 24 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142661 | Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142700 | Toxicity in Sprague-Dawley rat assessed as increase in minute volume at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142744 | Toxicity in dog assessed as macroscopic observation at 3 to 30 mg/kg/day, po qd administered for 4 weeks measured after 2 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142725 | Toxicity in male rat assessed as extramedullary hematopoiesis in spleen at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142737 | Cmax in male rat at 50 mg/kg/day, po qd after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142658 | Inhibition of VEGFR2 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139882 | Drug metabolism in po dosed rat urine assessed as formation of (4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methanol by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142608 | Inhibition of ALK3 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1256659 | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142628 | Inhibition of PDGFR-alpha V561D mutant (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142623 | Inhibition of MINK1 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142699 | Toxicity in Sprague-Dawley rat assessed as increase in tidal volume at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142636 | Inhibition of RIPK2 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142643 | Inhibition of VEGFR1 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1139883 | Drug metabolism in po dosed rat plasma assessed as formation of (4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methanol by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142728 | Toxicity in female rat assessed as ovarian atrophy at 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142642 | Inhibition of TGFbetaR2 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1256661 | Selectivity index, ratio of IC50 for human recombinant p38alpha to IC50 for human recombinant ALK5 | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142726 | Toxicity in male rat assessed as subphyseal hyperostosis in femur at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142672 | Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate at 10 uM incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1256660 | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142749 | Toxicity in Sprague-Dawley rat assessed as partially or completely closed eyelids at 1000 mg/kg, po after 1 to 6 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142704 | Toxicity in Sprague-Dawley rat assessed as effect on clinical observations at 10 to 100 mg/kg, po | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142677 | Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142680 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate at 10 uM incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142659 | Selectivity index, ratio of IC50 for VEGFR2 (unknown origin) to IC50 for ALK5 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142657 | Selectivity index, ratio of IC50 for RIPK2 (unknown origin) to IC50 for ALK5 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142703 | Toxicity in Sprague-Dawley rat assessed as mortality at 10 to 100 mg/kg, po | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142597 | Solubility of the compound in aqueous buffer at pH 6.8 after 24 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142734 | Toxicity in po dosed male rat administered qd for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142624 | Inhibition of MINK1 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142663 | Competitive inhibition of ALK5 (unknown origin) by Michaelis-Menten plot analysis in presence of ATP | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1634303 | Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
| Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| AID1142723 | Toxicity in male rat assessed as panlobular hypertrophy in liver at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142644 | Inhibition of VEGFR1 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142640 | Inhibition of TGFbetaR2 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1733254 | Inhibition of recombinant human p38alpha expressed in Escherichia coli assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors. |
| AID1142732 | Toxicity in female rat assessed as subphyseal hyperostosis in femur at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142639 | Inhibition of TGFbetaR2 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142717 | Cytotoxicity against CHO cells assessed as polyploid cells | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142748 | Cmax in dog at 30 mg/kg/day, po qd measured on day 28 | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142673 | Inhibition of CYP2C9 in human liver microsomes using tolbutamide as substrate incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142720 | Cytotoxicity against CHO cells assessed as polyploid cells in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1534896 | Inhibition of TGFBR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1142619 | Inhibition of MAP4K4 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1563852 | Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| AID1139884 | Drug metabolism in po dosed rat feces assessed as formation of (4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methanol by LC-MS analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase. |
| AID1142635 | Inhibition of RIPK2 (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142621 | Inhibition of MAP4K4 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142707 | Toxicity in po dosed Sprague-Dawley rat assessed as arousal in activity after 24 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142691 | Cardiotoxicity in po dosed beagle dog assessed as effect on heart rate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142716 | Mutagenic activity in Escherichia coli WP2 uvrA at 50 to 5000 ug/plate in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142740 | Toxicity in dog assessed as soft and watery feces at 30 mg/kg/day, po qd administered for 4 weeks measured after 2 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1634302 | Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
| Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors. |
| AID1142719 | Cytotoxicity against CHO cells assessed as aberrant metaphase in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1563853 | Selectivity index, ratio of IC50 for human recombinant untagged p38alpha expressed in Escherichia coli to IC50 for human recombinant GST-tagged ALK5 expressed in Sf9 insect cells | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives. |
| AID1142681 | Inhibition of human ERG channel expressed in HEK293 cells at 1 uM after 3 to 5.7 mins by whole-cell patch clamp technique | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142617 | Inhibition of ALK4 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142722 | Genotoxicity in Sprague-Dawley rat assessed as micronucleated polychromatic erythrocyte formation in bone marrow at 500 to 2000 mg/kg, po | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142708 | Mutagenic activity in Salmonella typhimurium TA100 at 50 to 5000 ug/plate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142718 | Cytotoxicity against CHO cells assessed as endoreduplicated cells | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142627 | Inhibition of PDGFR-alpha V561D mutant (unknown origin) assessed as residual activity at 0.01 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142656 | Inhibition of RIPK2 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142607 | Inhibition of ALK2 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142650 | Inhibition of VEGFR2 (unknown origin) assessed as residual activity at 10 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142743 | Toxicity in dog assessed as effect on clinical chemistry at 3 to 30 mg/kg/day, po qd administered for 4 weeks measured after 2 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142629 | Inhibition of PDGFR-alpha V561D mutant (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142692 | Cardiotoxicity in po dosed beagle dog assessed as effect on blood pressure | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142671 | Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142688 | Toxicity in po dosed beagle dog assessed as effect on body weight | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142733 | Toxicity in female rat assessed as growth plate thickening in sternum at 10 to 50 mg/kg/day, po qd administered for 4 weeks measured after 4 weeks | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142693 | Toxicity in Sprague-Dawley rat assessed as mortality at 1000 mg/kg, po | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142678 | Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate at 10 uM incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142676 | Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate at 10 uM incubated for 5 mins prior to substrate addition measured after 10 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142684 | Inhibition of human ERG channel expressed in HEK293 cells at 100 uM after 3 to 5.7 mins by whole-cell patch clamp technique | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142687 | Toxicity in po dosed beagle dog assessed as effect on clinical observation | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142645 | Inhibition of VEGFR1 (unknown origin) assessed as residual activity at 1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142702 | Cytotoxicity against CHO cells assessed as aberrant metaphase | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142689 | Toxicity in po dosed beagle dog assessed as effect on body temperature | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142610 | Inhibition of ALK6 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1142648 | Inhibition of VEGFR2 (unknown origin) assessed as residual activity at 0.1 uM by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1345571 | Human activin A receptor type 1B (Type I receptor serine/threonine kinases) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1345533 | Human transforming growth factor beta receptor 1 (Type I receptor serine/threonine kinases) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |