| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| 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. |
| 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. |
| AID683118 | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID683117 | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID683121 | Selectivity index, ratio of IC50 for human recombinant p38alpha to IC50 for human recombinant ALK5 | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID339538 | Inhibition of GST fused human recombinant ALK5 expressed in Sf9 cells by radioisotopic protein kinase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase. |
| 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/ |
| 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/ |
| AID622804 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGFbeta-induced p3TP-luciferase reporter activity at 100 nM relative to control | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID622807 | Oral bioavailability in rat at 50.3 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID339537 | Inhibition of human recombinant p38alpha MAPK expressed in Escherichia coli by radioisotopic protein kinase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase. |
| AID592902 | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID488282 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGF-beta-induced SBE-luciferase reporter activity at 0.1 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID1142591 | Selectivity for ALK5 (unknown origin) over p38alpha (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/ |
| AID1142589 | Oral bioavailability in mouse | 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/ |
| AID622805 | Oral bioavailability in dog at 5.5 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID1545186 | Drug elimination in human kidney | 2019 | Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
| An insight into medicinal chemistry of anticancer quinoxalines. |
| AID1139867 | Selectivity index, ratio of IC50 for recombinant human p38-alpha to IC50 for GST-fused recombinant human ALK5 | 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. |
| AID622811 | Selectivity index, ratio of IC50 for human recombinant p38alpha to IC50 human recombinant GST-fused ALK5 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID490196 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGF-beta-induced SBE-luciferase reporter activity at 0.1 uM after 18 to 24 hrs by luminescence assay relative to control | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| 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/ |
| AID615269 | Selectivity index, ratio of IC50 for human recombinant p38alpha to IC50 for human recombinant ALK5 | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| 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/ |
| AID488597 | Metabolic stability assessed as 3-((4-(2-hydroxyquinoxalin- 6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)benzamide or 3-((4-(3-hydroxyquinoxalin-6-yl)-5-(6-methylpyridin-2-yl)- 1H-imidazol-2-yl)methyl)benzamide) levels at 120 uM by HPLC analysis | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID622808 | Oral bioavailability in mouse at 50.3 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID683120 | Inhibition of human ALK5 activity in human HaCaT cells expressing p3TP-luciferase reporter construct assessed as TGFbeta-induced p3TP-luciferase reporter activity at 30 nM relative to control | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID488281 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGF-beta-induced p3TP-luciferase reporter activity at 0.1 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID488280 | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID615270 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGFbeta-induced p3TP-luciferase reporter activity at 0.1 uM after 24 hrs by luminescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| 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/ |
| AID592903 | Selectivity index, ratio of IC50 for human recombinant p38alpha to IC50 for human recombinant ALK5 | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID615320 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGFbeta-induced p3TP-luciferase reporter activity after 24 hrs by luminescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID488283 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGF-beta-induced ARE-luciferase reporter activity at 0.1 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID1139868 | Inhibition of ALK5 in human HaCaT cells assessed as remaining TGF-beta1-induced p3TP-luciferase reporter gene expression at 0.03 uM after 24 hrs by luminometric analysis relative to control | 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. |
| AID622809 | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID488519 | Metabolic stability assessed as 3-((4-(2-hydroxyquinoxalin- 6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)benzamide or 3-((4-(3-hydroxyquinoxalin-6-yl)-5-(6-methylpyridin-2-yl)- 1H-imidazol-2-yl)methyl)benzamide) levels at 120 uM by HPLC analysis | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID1139865 | Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay | 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. |
| 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/ |
| AID615267 | Inhibition of human recombinant GST-fused ALK5 expressed in insect Sf9 cells using casein as substrate by radiometric kinase assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID490195 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGF-beta-induced ARE-luciferase reporter activity at 0.1 uM after 18 to 24 hrs by luminescence assay relative to control | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID1534896 | Inhibition of TGFBR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Targeting the immunity protein kinases for immuno-oncology. |
| AID1142587 | Oral bioavailability in dog | 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/ |
| AID488520 | Metabolic stability assessed as 3-((4-(2-hydroxyquinoxalin- 6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)benzamide or 3-((4-(3-hydroxyquinoxalin-6-yl)-5-(6-methylpyridin-2-yl)- 1H-imidazol-2-yl)methyl)benzamide) levels at 120 uM by HPLC analysis | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID592901 | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID622810 | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID1142590 | Oral bioavailability in rat | 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/ |
| AID622806 | Oral bioavailability in rhesus monkey at 5.5 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| AID592904 | Inhibition of human recombinant ALK5 activity in human HaCaT cells assessed as TGFbeta-induced p3TP-luciferase reporter activity at 0.1 uM relative to control | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| 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/ |
| 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/ |
| AID488521 | Metabolic stability assessed as 3-((4-(2-hydroxyquinoxalin- 6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)benzamide or 3-((4-(3-hydroxyquinoxalin-6-yl)-5-(6-methylpyridin-2-yl)- 1H-imidazol-2-yl)methyl)benzamide) levels at 120 uM by HPLC analysis | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID1142588 | Oral bioavailability in monkey | 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/ |
| AID490112 | Inhibition of human ALK5 activity in human HaCaT cells assessed as inhibition of TGF-beta-induced p3TP-luciferase reporter activity at 0.1 uM after 18 to 24 hrs by luminescence assay relative to control | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. |
| AID1139866 | Inhibition of recombinant human p38-alpha expressed in Escherichia coli using ATF2 as substrate by radioisotope-based assay | 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. |
| 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/ |
| 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/ |
| AID615268 | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by radiometric kinase assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |