Assay ID | Title | Year | Journal | Article |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
| Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347154 | Primary screen GU AMC 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. |
AID384896 | Cytotoxicity against human LCLC-97TM1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384186 | Cytotoxicity against human NCI-H2196 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653852 | Inhibition of PKA assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653232 | Inhibition of LRRK2 phosphorylation at Ser935 in C57BL/6 mouse brain at 10 to 50 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID361001 | Cell cycle arrest in human Karpas299 cells by accumulation in S phase at 25 nM after 72 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384663 | Cytotoxicity against human NCI-H2009 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384197 | Cytotoxicity against human NCI-H441 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653438 | Inhibition of NEK2a assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653825 | Inhibition of MKK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384410 | Cytotoxicity against human RERF-LC-MS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653796 | Inhibition of GCK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384636 | Cytotoxicity against human MSTO-211H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384842 | Cytotoxicity against human HuCCT1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384390 | Cytotoxicity against human Panc03.27 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384651 | Cytotoxicity against human NCI-H1693 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653426 | Inhibition of MINK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384175 | Cytotoxicity against human UMC11 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384660 | Cytotoxicity against human NCI-H1944 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384844 | Cytotoxicity against human HUP-T3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383089 | Inhibition of KDR by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383866 | Cytotoxicity against human EFM192A cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384656 | Cytotoxicity against human NCI-H1792 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653802 | Inhibition of IGF-1R assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360945 | Bioavailability in human Karpas299 cells xenografted SCID beige mouse at 20 mg/kg | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383633 | Cytotoxicity against human COLO 320DM cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653853 | Inhibition of PKBalpha assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384131 | Cytotoxicity against human SNU398 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384146 | Cytotoxicity against human SW1573 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653636 | Inhibition of CK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653225 | Inhibition of LRRK2 phosphorylation at Ser935 in C57BL/6 mouse kidney at 10 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360956 | Inhibition of mouse wild type BaF3/WT Luc+ cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID1191197 | Inhibition of ALK (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
AID1369784 | Induction of ALK degradation in human NCI-H3122 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID384681 | Cytotoxicity against human Hs 257.T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1416442 | Inhibition of wild type non-phosphorylated N-terminal His6-tagged FGFR4 (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
AID383627 | Cytotoxicity against human CL11 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383937 | Cytotoxicity against human SK-LU-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653408 | Inhibition of IR assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383093 | Inhibition of PDGFRbeta by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384687 | Cytotoxicity against human Hs 746T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653444 | Inhibition of p38delta MAPK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384891 | Cytotoxicity against human KYSE510 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383602 | Cytotoxicity against human C170 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384846 | Cytotoxicity against human IGR1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383890 | Cytotoxicity against human H3255 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384867 | Cytotoxicity against human KG-1-C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID757926 | Activity at insulin receptor in mouse assessed as effect on insulin level up to 100 mg/kg by oral glucose tolerance test | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID384148 | Cytotoxicity against human SW1990 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653847 | Inhibition of PDK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384693 | Cytotoxicity against human HTC-C3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653602 | Inhibition of S6K1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384620 | Cytotoxicity against human MES-SA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653804 | Inhibition of IKKepsilon assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383094 | Inhibition of Ret by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1369764 | Antiproliferative activity against human KARPAS299 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID384368 | Cytotoxicity against human Nthyl-ori 3-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360969 | Inhibition of Tel-fused ALK kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID360943 | Inhibition of NPM-ALK in human Karpas299 cells at 50 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384203 | Cytotoxicity against human NCI-H647 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653810 | Inhibition of JNK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360968 | Inhibition of Tel-fused TRKB kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384638 | Cytotoxicity against human NB69 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384843 | Cytotoxicity against human huH-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360974 | Inhibition of Tel-fused Bmx kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID1915686 | Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation. |
AID383620 | Cytotoxicity against human Capan1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1310842 | Protein binding in rat plasma | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID360973 | Inhibition of Tel-fused Lyn kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653643 | Inhibition of DYRK3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383109 | Inhibition of ALK by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383932 | Cytotoxicity against human SK-BR3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384176 | Cytotoxicity against human UM-UC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361012 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 3 mg/kg, po once daily after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653800 | Inhibition of HIPK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653431 | Inhibition of MLK3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID361014 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 10 mg/kg, po once daily after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384140 | Cytotoxicity against human SW1116 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383920 | Cytotoxicity against human HeLa.P3(s) cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1369763 | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID384650 | Cytotoxicity against human NCI-H1666 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654015 | Inhibition of TBK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653827 | Inhibition of MLK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654017 | Inhibition of TIE2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384152 | Cytotoxicity against human SW1710 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653850 | Inhibition of PIM2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653382 | Inhibition of CSK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383591 | Cytotoxicity against human BFTC905 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384857 | Cytotoxicity against human Ishikawa 02 ER cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384621 | Cytotoxicity against human MEL-SA/Dx-5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653650 | Inhibition of EPH-B3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384135 | Cytotoxicity against human SU.86.86 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653401 | Inhibition of HER4 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653622 | Inhibition of ABL assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID767460 | Inhibition of CSF1R (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Selectivity data: assessment, predictions, concordance, and implications. |
AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383091 | Inhibition of Lck by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384877 | Cytotoxicity against human KP3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384402 | Cytotoxicity against human PL45 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653628 | Inhibition of BRSK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653235 | Inhibition of AMPK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383587 | Cytotoxicity against human B-CPAP cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383889 | Cytotoxicity against human GTL16 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID361004 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 3 mg/kg, po once daily after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653842 | Inhibition of p38gamma MAPK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383396 | Cytotoxicity against human 786-O cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383399 | Cytotoxicity against human A172 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653412 | Inhibition of JAK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653601 | Inhibition of RSK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384422 | Cytotoxicity against human LNZTA3WT11 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653436 | Inhibition of MST2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID654028 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser910 expressed in HEK293 cells at 0.1 to 0.3 uM after 90 mins by immunoblot analysis relative to LRRK2-IN1 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384429 | Cytotoxicity against human Lu135 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653817 | Inhibition of MARK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383638 | Cytotoxicity against human COLO 858 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1310844 | Aqueous solubility of the compound at physiological pH | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID383902 | Cytotoxicity against human HCC366 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653428 | Inhibition of MKK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384677 | Cytotoxicity against human HOP92 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654018 | Inhibition of TLK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1369789 | Antiproliferative activity against human CHLA20 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID360999 | Induction of apoptosis in human Karpas299 cells by annexin V assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653799 | Inhibition of HIPK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384885 | Cytotoxicity against human KYSE220 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653396 | Inhibition of ERK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384412 | Cytotoxicity against human RKN cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384405 | Cytotoxicity against human RCM1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654009 | Inhibition of Src assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383389 | Cytotoxicity against human 201T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653383 | Inhibition of DAPK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383918 | Cytotoxicity against human HeLa TG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383912 | Cytotoxicity against human HDQ-P1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384872 | Cytotoxicity against human KMRC20 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384200 | Cytotoxicity against human NCI-H522 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384366 | Cytotoxicity against human NCI-N87 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384443 | Cytotoxicity against human MDA-MB-361 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625058 | Binding constant for VRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384367 | Cytotoxicity against human NH6 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384144 | Cytotoxicity against human SW1463 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653198 | Inhibition of LRRK2 G2019S and A2016T mutant phosphorylation at Ser910 expressed in HEK293 cells at 1 to 3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID361008 | Toxicity in human Karpas299 cells xenografted in SCID beige mouse at 10 mg/kg, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384631 | Cytotoxicity against human MKN74 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384427 | Cytotoxicity against human LS180 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383601 | Cytotoxicity against human BxPC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384628 | Cytotoxicity against human MKN28 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653226 | Inhibition of LRRK2 phosphorylation at Ser910 in C57BL/6 mouse spleen at 10 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360984 | Inhibition of InsR phosphorylation in rat H4-2E cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653430 | Inhibition of MLK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360992 | Inhibition of STAT5 phosphorylation in human SUDHL1 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1310804 | Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653598 | Inhibition of RIPK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383604 | Cytotoxicity against human C33A cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID757923 | Selectivity ratio of IC50 for TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells to IC50 for NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID653814 | Inhibition of LKB1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653641 | Inhibition of DYRK1A assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653839 | Inhibition of p38alpha MAPK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383106 | Inhibition of FLT3 by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360960 | Inhibition of Tel-fused FLT3 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383637 | Cytotoxicity against human COLO 857 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384678 | Cytotoxicity against human HOS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384391 | Cytotoxicity against human Panc04.03 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653192 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser910 expressed in HEK293 cells after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384627 | Cytotoxicity against human MKN1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360965 | Inhibition of Tel-fused RET kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653619 | Inhibition of VEGFR assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384202 | Cytotoxicity against human NCI-H630 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384132 | Cytotoxicity against human SNU449 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384182 | Cytotoxicity against human NCI-H2122 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360979 | Inhibition of FLT3 kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653404 | Inhibition of HIPK3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384444 | Cytotoxicity against human MDA-MB-415 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384397 | Cytotoxicity against human PA-TU-8988T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360987 | Inhibition of STAT5 phosphorylation in human Karpas299 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383625 | Cytotoxicity against human CFPAC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383630 | Cytotoxicity against human CL40 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383590 | Cytotoxicity against human BEN cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360989 | Inhibition of STAT3 phosphorylation in human Karpas299 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654014 | Inhibition of TAO1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383644 | Cytotoxicity against human COLO 680N cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383090 | Inhibition of c-Kit by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384442 | Cytotoxicity against human MDA-MB-231 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653819 | Inhibition of MARK3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384893 | Cytotoxicity against human KYSE70 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361005 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 10 mg/kg, po once daily after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383892 | Cytotoxicity against human H69V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654008 | Inhibition of SmMLCK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653587 | Inhibition of PIM3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653414 | Inhibition of JNK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1562813 | Inhibition of FLT3 ITD mutant (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. |
AID383100 | Inhibition of FGFR3 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384899 | Cytotoxicity against human LN229 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653863 | Inhibition of ROCK 2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384911 | Cytotoxicity against human YAPC cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1369786 | Induction of ALK degradation in human NCI-H3122 cells assessed as decrease in ALK phosphorylation at Y1604 at 250 nM measured over 6 to 48 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653635 | Inhibition of CHK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383387 | Cytotoxicity against human 143B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384634 | Cytotoxicity against human MRC9 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383582 | Cytotoxicity against human AGS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653824 | Inhibition of MKK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653240 | Inhibition of BRSK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384435 | Cytotoxicity against human M14 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360950 | Inhibition of NPM-ALK autophosphorylation in human Karpas299 cells after 4 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653209 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser935 in mouse 3T3 cells after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360978 | Inhibition of Tie2 kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID361006 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 3 mg/kg, po once daily after 4 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653590 | Inhibition of PKBbeta assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384154 | Cytotoxicity against human SW620 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384865 | Cytotoxicity against human KATO II cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384434 | Cytotoxicity against human M059J cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383632 | Cytotoxicity against human COLO 205 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384632 | Cytotoxicity against human ML1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383906 | Cytotoxicity against human HCC70 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384371 | Cytotoxicity against human NUGC4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653805 | Inhibition of IR assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384377 | Cytotoxicity against human OE33 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383878 | Cytotoxicity against human FU97 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383648 | Cytotoxicity against human COLO 849 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384158 | Cytotoxicity against human T.T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383096 | Inhibition of Syk by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654025 | Inhibition of ZAP70 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383624 | Cytotoxicity against human CCK81 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383392 | Cytotoxicity against human 42-MG-BA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384389 | Cytotoxicity against human Panc02.03 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653809 | Inhibition of JAK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384162 | Cytotoxicity against human T84 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653846 | Inhibition of PAK6 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383928 | Cytotoxicity against human SF295 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1310803 | Inhibition of human InsR using myelin basic protein as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653638 | Inhibition of CLK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384376 | Cytotoxicity against human OE21 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384126 | Cytotoxicity against human SK-N-AS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383593 | Cytotoxicity against human BHT101 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383384 | Cytotoxicity against human 5637 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653859 | Inhibition of PLK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383097 | Inhibition of Tie2 by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383583 | Cytotoxicity against human ASH3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654016 | Inhibition of TESK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384662 | Cytotoxicity against human NCI-H1975 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384153 | Cytotoxicity against human SW527 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383629 | Cytotoxicity against human CL34 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384125 | Cytotoxicity against human SK-MES1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383594 | Cytotoxicity against human BIC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383628 | Cytotoxicity against human CL14 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384644 | Cytotoxicity against human NCI-H1568 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383935 | Cytotoxicity against human SKG-IIIb cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1845591 | Binding affinity to NUAK2 (unknown origin) assessed as dissociation constant | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development and Therapeutic Potential of NUAKs Inhibitors. |
AID383870 | Cytotoxicity against human EGI1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1310846 | Lipophilicity, logD of the compound at pH 7 | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID384647 | Cytotoxicity against human NCI-H1623 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360976 | Inhibition of Tel-fused ZAP70 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653427 | Inhibition of MKK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383605 | Cytotoxicity against human C-4 I cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384165 | Cytotoxicity against human TASK1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360954 | Decrease in ALK phosphorylation in human SUDHL1 cells after 4 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383875 | Cytotoxicity against human FTC133 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383609 | Cytotoxicity against human Caki1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653221 | Inhibition of LRRK2 phosphorylation at Ser935 in C57BL/6 mouse kidney at 50 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653599 | Inhibition of ROCK 2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383888 | Cytotoxicity against human GP5d cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653593 | Inhibition of PKCgamma assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384188 | Cytotoxicity against human NCI-H2286 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384675 | Cytotoxicity against human HMCB cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384130 | Cytotoxicity against human SNU182 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384433 | Cytotoxicity against human LUDLU1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383901 | Cytotoxicity against human HCC1954 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384378 | Cytotoxicity against human ONCO-DG-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384908 | Cytotoxicity against human WM278 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624986 | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384438 | Cytotoxicity against human MCF-7/ADR cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653418 | Inhibition of MAPKAPK2- assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384163 | Cytotoxicity against human T98G cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383603 | Cytotoxicity against human C32 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653807 | Inhibition of IRAK4 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653594 | Inhibition of PKD1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383907 | Cytotoxicity against human HCC78 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360944 | Elimination half life in human Karpas299 cells xenografted SCID beige mouse at 20 mg/kg, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID360955 | Decrease in ALK phosphorylation in mouse Ba/F3 NPM-ALK cells after 4 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653589 | Inhibition of PKBalpha assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384416 | Cytotoxicity against human RT-112 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653439 | Inhibition of NEK6 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384691 | Cytotoxicity against human HT29 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653411 | Inhibition of IRR assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653854 | Inhibition of PKBbeta assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1915687 | Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation. |
AID383885 | Cytotoxicity against human GCT cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653862 | Inhibition of RIPK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1310841 | Protein binding in human plasma | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID384874 | Cytotoxicity against human KP-1N cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384916 | Cytotoxicity against human SK-N-SH cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653608 | Inhibition of SYK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383345 | Inhibition of Syk | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384856 | Cytotoxicity against human Ishikawa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383395 | Cytotoxicity against human 769-P cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383651 | Cytotoxicity against human COR-L23 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384665 | Cytotoxicity against human NCI-H2029 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1369839 | Induction of EML4-ALK C1156Y mutant (unknown origin) degradation expressed in mouse BA/F3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653194 | Inhibition of wild-type LRRK2 phosphorylation at Ser910 expressed in HEK293 cells at 0.1 to 0.3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384413 | Cytotoxicity against human RMG-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384673 | Cytotoxicity against human HLE cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1369787 | Induction of ALK degradation in human NCI-H3122 cells assessed as decrease in STAT3 phosphorylation at Y705 at 250 nM measured over 6 to 48 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID383867 | Cytotoxicity against human EFM-192B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383087 | Inhibition of FGFR1 by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361017 | Antilymphomal activity against human Karpas299 cells xenografted in SCIDbeige mouse assessed as reduction in CD30 expression in lymph nodes after 3.5 weeks of infection at 10 mg/kg for 3 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384385 | Cytotoxicity against human OVMIU cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624981 | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384134 | Cytotoxicity against human STC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383576 | Cytotoxicity against human A375.S2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384136 | Cytotoxicity against human SUIT2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1137609 | Inhibition of purified recombinant ALK (unknown origin) after 60 mins by ELISA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
AID653413 | Inhibition of JNK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383652 | Cytotoxicity against human DAN-G cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383584 | Cytotoxicity against human AsPC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653400 | Inhibition of GSK3b assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653613 | Inhibition of TIE2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383898 | Cytotoxicity against human HCC15 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653419 | Inhibition of MAPKAP-K3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384394 | Cytotoxicity against human PANC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653611 | Inhibition of TBK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383088 | Inhibition of Flt1 by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384879 | Cytotoxicity against human KP4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384365 | Cytotoxicity against human NCI-H838 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384393 | Cytotoxicity against human Panc10.05 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384860 | Cytotoxicity against human JHH4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384161 | Cytotoxicity against human T47D cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653387 | Inhibition of EF2K assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360995 | Inhibition of PI3K/Akt signaling in human Karpas299 cells assessed as Akt phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383385 | Cytotoxicity against human 1205Lu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360997 | Induction of apoptosis in human SUDHL1 cells at 50 nM after 48 hrs by annexin V assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653600 | Inhibition of RSK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653831 | Inhibition of MPSK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383588 | Cytotoxicity against human BE(2)-C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360986 | Inhibition of Akt phosphorylation in rat H4-2E cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383873 | Cytotoxicity against human EVSA-T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383634 | Cytotoxicity against human COLO 741 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384692 | Cytotoxicity against human HT3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653840 | Inhibition of p38beta MAPK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383308 | Inhibition of InsR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383922 | Cytotoxicity against human SBC5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383934 | Cytotoxicity against human SKG-IIIa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384876 | Cytotoxicity against human KP2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653851 | Inhibition of PIM3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384878 | Cytotoxicity against human KP-3L cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653844 | Inhibition of PAK4 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID775337 | Binding affinity to human MLK3 | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384616 | Cytotoxicity against human MDST8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654013 | Inhibition of TAK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653423 | Inhibition of MARK4 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384883 | Cytotoxicity against human KYSE150 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653133 | Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360970 | Inhibition of Tel-fused JAK2 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360966 | Inhibition of Tel-fused RON kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID360991 | Inhibition of STAT5 phosphorylation in mouse Ba/F3 NPM-ALK cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383621 | Cytotoxicity against human Capan2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384375 | Cytotoxicity against human OE19 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653241 | Inhibition of BRSK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1416440 | Inhibition of phosphorylated FGFR2 (406 to 821 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
AID384151 | Cytotoxicity against human SW900 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384657 | Cytotoxicity against human NCI-H1793 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383595 | Cytotoxicity against human BICR 78 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653433 | Inhibition of MNK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384641 | Cytotoxicity against human NCI-H1435 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653394 | Inhibition of EPH-B4 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653830 | Inhibition of MNK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384166 | Cytotoxicity against human TCO1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384398 | Cytotoxicity against human PC14 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653623 | Inhibition of AMPK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384415 | Cytotoxicity against human RPMI-7951 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1205046 | Inhibition of ACK1 Tyr284 phosphorylation in human LAPC4 cells at 5 uM after 16 hrs by immunoblotting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
| Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. |
AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID758043 | Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID360952 | Inhibition of NPM-ALK autophosphorylation in mouse Ba/F3 NPM-ALK cells after 4 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384399 | Cytotoxicity against human PC-3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383908 | Cytotoxicity against human HCC827cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383891 | Cytotoxicity against human H4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653616 | Inhibition of TSSK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653384 | Inhibition of DYRK1A assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384395 | Cytotoxicity against human PA-TU-8902 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383098 | Inhibition of TrkC by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653208 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser910 in mouse 3T3 cells after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1845567 | Inhibition of wild type ALK (unknown origin) | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development and Therapeutic Potential of NUAKs Inhibitors. |
AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653640 | Inhibition of DAPK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383049 | Inhibition of Bmx by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383101 | Inhibition of Fes | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384179 | Cytotoxicity against human VMRC-LCD cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653820 | Inhibition of MARK4 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383585 | Cytotoxicity against human AU565 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384862 | Cytotoxicity against human JR 013 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384170 | Cytotoxicity against human U118 MG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653620 | Inhibition of YES1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653415 | Inhibition of JNK3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383626 | Cytotoxicity against human ChaGo-K-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653588 | Inhibition of PKA assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383938 | Cytotoxicity against human SK-MEL-3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653443 | Inhibition of p38beta MAPK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1350814 | Inhibition of TEL-fused EGFR (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID384381 | Cytotoxicity against human OVCAR5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID642895 | Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID654022 | Inhibition of TTK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID654020 | Inhibition of TSSK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384851 | Cytotoxicity against human IM95 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653806 | Inhibition of IRAK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360953 | Decrease in ALK phosphorylation in human Karpas299 cells after 4 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384884 | Cytotoxicity against human KYSE180 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384900 | Cytotoxicity against human LN405 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384661 | Cytotoxicity against human NCI-H196 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653798 | Inhibition of HER4 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384139 | Cytotoxicity against human SW1088 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653630 | Inhibition of BTK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384646 | Cytotoxicity against human NCI-H1581 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653245 | Inhibition of CDK2-Cyclin A assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653591 | Inhibition of PKCalpha assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653385 | Inhibition of DYRK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383900 | Cytotoxicity against human HCC1937 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384684 | Cytotoxicity against human Hs 633T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1579880 | Inhibition of EML4/ALK in human NCI-H3122 cells | | | |
AID383085 | Inhibition of EphA3 by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383635 | Cytotoxicity against human COLO 792 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653210 | AUClast in Swiss albino mouse plasma at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384913 | Cytotoxicity against human ZR-75-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384645 | Cytotoxicity against human NCI-H1573 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653651 | Inhibition of EPH-B4 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID642891 | Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID653803 | Inhibition of IKKbeta assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384184 | Cytotoxicity against human NCI-H2170 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653612 | Inhibition of TESK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653224 | Inhibition of LRRK2 phosphorylation at Ser910 in C57BL/6 mouse kidney at 10 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653645 | Inhibition of EIF2AK3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384384 | Cytotoxicity against human OVKATE cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653410 | Inhibition of IRAK4 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384648 | Cytotoxicity against human NCI-H1650 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653586 | Inhibition of PIM2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1137615 | Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
AID653399 | Inhibition of GCK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384870 | Cytotoxicity against human KMH2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653605 | Inhibition of Src assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653637 | Inhibition of CK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID361007 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 10 mg/kg, po once daily after 4 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384150 | Cytotoxicity against human SW780 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383575 | Cytotoxicity against human A-375 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384441 | Cytotoxicity against human MDA-MB-157 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383649 | Cytotoxicity against human COR-L 105 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384168 | Cytotoxicity against human TGW cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384400 | Cytotoxicity against human PC-3[JPC-3] cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384189 | Cytotoxicity against human NCI-H23 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384640 | Cytotoxicity against human NCI-H1299 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653242 | Inhibition of BTK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653442 | Inhibition of p38alpha MAPK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360977 | Inhibition of Tel-fused Syk kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653448 | Inhibition of PAK5 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1369838 | Induction of EML4-ALK G1202R mutant (unknown origin) degradation expressed in mouse BA/F3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653633 | Inhibition of CDK2-Cyclin A assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653220 | Inhibition of LRRK2 phosphorylation at Ser910 in C57BL/6 mouse kidney at 50 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383099 | Inhibition of Bmx | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383607 | Cytotoxicity against human Ca Ski cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653818 | Inhibition of MARK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653234 | Inhibition of ABL assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653190 | Inhibition of wild-type LRRK2 phosphorylation at Ser910 expressed in HEK293 cells after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384424 | Cytotoxicity against human LOU-NH91 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384430 | Cytotoxicity against human LU99A cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384137 | Cytotoxicity against human SVG p12 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384145 | Cytotoxicity against human SW156 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383860 | Cytotoxicity against human DMS 53 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384198 | Cytotoxicity against human NCI-H460 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383608 | Cytotoxicity against human Caco-2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383919 | Cytotoxicity against human HeLa TG Cap cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383926 | Cytotoxicity against human SCLC21H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384615 | Cytotoxicity against human MDA-MB-468 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1310802 | Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID384626 | Cytotoxicity against human MIA PaCa-2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653424 | Inhibition of MEKK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360975 | Inhibition of Tel-fused Abl kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653647 | Inhibition of EPH-A4 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653446 | Inhibition of PAK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653238 | Inhibition of Aurora B assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383606 | Cytotoxicity against human C-4 II cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384419 | Cytotoxicity against human RVH-421 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384143 | Cytotoxicity against human SW1417 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384206 | Cytotoxicity against human NCI-H810 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360958 | Inhibition of Tel-fused Tie2 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384671 | Cytotoxicity against human HGC27 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384847 | Cytotoxicity against human IGR37 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384173 | Cytotoxicity against human U373 MG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653642 | Inhibition of DYRK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383879 | Cytotoxicity against human TMK1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1416438 | Inhibition of phosphorylated FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
AID653227 | Inhibition of LRRK2 phosphorylation at Ser935 in C57BL/6 mouse spleen at 10 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653801 | Inhibition of HIPK3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384195 | Cytotoxicity against human NCI-H322 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653197 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser935 expressed in HEK293 cells at 1 to 3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653797 | Inhibition of GSK3b assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384157 | Cytotoxicity against human SW948 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654006 | Inhibition of S6K1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383579 | Cytotoxicity against human A549 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384190 | Cytotoxicity against human NCI-H2342 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361013 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 5 mg/kg, po once daily after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1529863 | Inhibition AXL (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors. |
AID383862 | Cytotoxicity against human DU145 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360964 | Inhibition of Tel-fused FGFR1 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384142 | Cytotoxicity against human SW13 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384633 | Cytotoxicity against human MOG-G-UVW cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384423 | Cytotoxicity against human LNZTA3WT4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360980 | Inhibition of TRKB kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID759889 | Drug metabolism assessed as GSH adduct formation | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. |
AID1369762 | Inhibition of N-terminal GST-tagged human ALK (1058 to 1620 residues) expressed in baculovirus expression system using biotinylated gastrin peptide as substrate after 1 hr by TR-FRET assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID384159 | Cytotoxicity against human T.Tn cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384380 | Cytotoxicity against human OV1063 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383643 | Cytotoxicity against human SNU16 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384183 | Cytotoxicity against human NCI-H2135 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384901 | Cytotoxicity against human VMRC-RCW cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384177 | Cytotoxicity against human UO31 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383921 | Cytotoxicity against human SBC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654004 | Inhibition of RSK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID642896 | Cytotoxicity against human SMS-KCN cells expressing ALK R1275Q mutant | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID653214 | Half life in Swiss albino mouse at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384204 | Cytotoxicity against human NCI-H661 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384382 | Cytotoxicity against human OVCAR8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383592 | Cytotoxicity against human BFTC909 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653794 | Inhibition of ERK8 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383886 | Cytotoxicity against human GMS10 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384196 | Cytotoxicity against human NCI-H358 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653603 | Inhibition of SGK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384895 | Cytotoxicity against human LCLC-103H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384191 | Cytotoxicity against human NCI-H2347 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360971 | Inhibition of Tel-fused TYK2 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653205 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser935 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384409 | Cytotoxicity against human RERF-LC-KJ cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653397 | Inhibition of ERK8 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383613 | Cytotoxicity against human CAL29 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384890 | Cytotoxicity against human KYSE50 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360967 | Inhibition of Tel-fused MET kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384639 | Cytotoxicity against human NCI-H1048 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384128 | Cytotoxicity against human SNG-M cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1529864 | Inhibition MER (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors. |
AID383887 | Cytotoxicity against human GOS3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1350813 | Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653644 | Inhibition of EF2K assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384169 | Cytotoxicity against human TYK-nu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653189 | Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384160 | Cytotoxicity against human T24 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383863 | Cytotoxicity against human DV 90 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1369788 | Antiproliferative activity against human SH-SY5Y cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID361015 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in NPM-ALK phosphorylation after 3.5 weeks of infection at 10 mg/kg for 3 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653609 | Inhibition of TAK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1310801 | Inhibition of human ALK using poly[Glu:Tyr] (4:1) as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384619 | Cytotoxicity against human MEL-JUSO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653402 | Inhibition of HIPK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653216 | Volume of distribution at steady state in Swiss albino mouse at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384614 | Cytotoxicity against human MDA-MB-453 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653191 | Inhibition of wild-type LRRK2 phosphorylation at Ser935 expressed in HEK293 cells after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653420 | Inhibition of MARK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384861 | Cytotoxicity against human JIMT1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383600 | Cytotoxicity against human thymidine kinase deficient Bu25 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653233 | Inhibition of LRRK2 phosphorylation at Ser910 in C57BL/6 mouse brain at 10 to 50 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384882 | Cytotoxicity against human KYSE140 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383647 | Cytotoxicity against human COLO 824 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384629 | Cytotoxicity against human MKN45 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384664 | Cytotoxicity against human NCI-H2023 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625081 | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653826 | Inhibition of MKK6 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1369837 | Induction of EML4-ALK L1196M mutant (unknown origin) degradation expressed in mouse BA/F3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID653239 | Inhibition of BRK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384669 | Cytotoxicity against human NCI-H2087 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653392 | Inhibition of EPH-B2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID758045 | Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID383650 | Cytotoxicity against human COR-L 23/CPR cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383394 | Cytotoxicity against human 647-V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383940 | Cytotoxicity against human SK-MES cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653403 | Inhibition of HIPK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653195 | Inhibition of wild-type LRRK2 phosphorylation at Ser935 expressed in HEK293 cells at 0.1 to 0.3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384909 | Cytotoxicity against human WM35 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361009 | Antilymphomal activity against mouse Ba/F3 BCR-ABL cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 10 mg/kg, po once daily after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383641 | Cytotoxicity against human COLO 678 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653621 | Inhibition of ZAP70 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653213 | AUClast in Swiss albino mouse brain at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653434 | Inhibition of MPSK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653812 | Inhibition of JNK3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384683 | Cytotoxicity against human Hs 578T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383882 | Cytotoxicity against human G401 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID758041 | Metabolic stability in human liver microsomes assessed as level of GSH adduct after 60 mins by LC-MS analysis relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383654 | Cytotoxicity against human DLD1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653196 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser910 expressed in HEK293 cells at 1 to 3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653845 | Inhibition of PAK5 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383095 | Inhibition of Src by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383086 | Inhibition of EphB4 by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653855 | Inhibition of PKCalpha assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384370 | Cytotoxicity against human NUGC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361016 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in downstream target STAT3 phosphorylation after 3.5 weeks of infection at 10 mg/kg for 3 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383596 | Cytotoxicity against human BT474 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384912 | Cytotoxicity against human YKG1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653211 | AUClast in Swiss albino mouse brain at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653447 | Inhibition of PAK4 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384431 | Cytotoxicity against human LU99B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654005 | Inhibition of RSK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384875 | Cytotoxicity against human KP-1NL cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384637 | Cytotoxicity against human MT3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653441 | Inhibition of OSR1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653416 | Inhibition of Lck assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384392 | Cytotoxicity against human Panc08.13 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360998 | Induction of apoptosis in human Karpas299 cells at 50 nM after 48 hrs by annexin V assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383874 | Cytotoxicity against human fR2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383884 | Cytotoxicity against human GAMG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653244 | Inhibition of CAMKKb assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1845590 | Binding affinity to NUAK1 (unknown origin) assessed as dissociation constant | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development and Therapeutic Potential of NUAKs Inhibitors. |
AID384690 | Cytotoxicity against human HT115 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383923 | Cytotoxicity against human SCaBER cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360990 | Inhibition of STAT3 phosphorylation in human SUDHL1 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383640 | Cytotoxicity against human COLO 320 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384676 | Cytotoxicity against human HMVII cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384407 | Cytotoxicity against human RERF-LC-Ad1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384854 | Cytotoxicity against human IPC298 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1369765 | Antiproliferative activity against human SU-DHL1 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653437 | Inhibition of MST4 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360982 | Inhibition of Syk kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384178 | Cytotoxicity against human VM-CUB1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653204 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser910 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360947 | Cytotoxicity against mouse parental Ba/F3 cells assessed as luciferase expression up to 1 uM after 2 to 3 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383896 | Cytotoxicity against human HBE4-E6E7-C1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360983 | Inhibition of recombinant InsR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384666 | Cytotoxicity against human NCI-H2030 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653388 | Inhibition of EIF2AK3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384649 | Cytotoxicity against human NCI-H1651 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384871 | Cytotoxicity against human KMRC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383939 | Cytotoxicity against human SK-MEL-30 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383877 | Cytotoxicity against human FTC238 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653829 | Inhibition of MNK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383343 | Inhibition of InsR by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653247 | Inhibition of CHK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384613 | Cytotoxicity against human MDA-MB-436 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653398 | Inhibition of FGF-R1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID654027 | Inhibition of wild-type LRRK2 phosphorylation at Ser935 expressed in HEK293 cells at 0.1 to 0.3 uM after 90 mins by immunoblot analysis relative to LRRK2-IN1 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384388 | Cytotoxicity against human PA1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1369790 | Antiproliferative activity against human CHLA20 cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID384652 | Cytotoxicity against human NCI-H1703 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653395 | Inhibition of ERK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360949 | Antiproliferative activity against human SUDHL1 cells assessed as luciferase expression after 72 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653217 | Ratio of AUClast in brain to plasma of Swiss albino mouse at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384850 | Cytotoxicity against human IHH4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653199 | Inhibition of LRRK2 G2019S and A2016T mutant phosphorylation at Ser935 expressed in HEK293 cells at 1 to 3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384898 | Cytotoxicity against human LN18 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384688 | Cytotoxicity against human Hs 894(E).Lu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384654 | Cytotoxicity against human NCI-H1755 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383915 | Cytotoxicity against human HeLa AG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653848 | Inhibition of PHK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383904 | Cytotoxicity against human HCC44 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1579879 | Inhibition of EML4/ALK in human NCI-H2228 cells | | | |
AID384622 | Cytotoxicity against human MEWO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653584 | Inhibition of PHK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384889 | Cytotoxicity against human KYSE450 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383617 | Cytotoxicity against human CAL-85-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383864 | Cytotoxicity against human EBC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383869 | Cytotoxicity against human EFO21 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360948 | Antiproliferative activity against human Karpas299 cells assessed as luciferase expression after 72 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID1350801 | Growth inhibition of human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID360962 | Inhibition of Tel-fused KDR kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384420 | Cytotoxicity against human S-117 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654021 | Inhibition of TTBK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653432 | Inhibition of MNK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID757924 | Activity at insulin receptor in mouse homeostasis model assessment of insulin resistance at 25 to 100 mg/kg, po for 7 days by oral glucose tolerance test | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID384428 | Cytotoxicity against human Lu-134-A-H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384439 | Cytotoxicity against human MC-IXC cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID642893 | Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID383386 | Cytotoxicity against human 1321N cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653861 | Inhibition of PRK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383865 | Cytotoxicity against human EFM19 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384141 | Cytotoxicity against human SW1271 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653391 | Inhibition of EPH-B1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360988 | Inhibition of STAT3 phosphorylation in mouse Ba/F3 NPM-ALK cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653607 | Inhibition of STK33 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654019 | Inhibition of TrkA assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1562814 | Inhibition of FLT3 D835Y mutant (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. |
AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383398 | Cytotoxicity against human 8505C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653219 | Oral bioavailability in Swiss albino mouse at 10 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384181 | Cytotoxicity against human VMRC-MELG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653407 | Inhibition of IKKepsilon assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383905 | Cytotoxicity against human HCC56 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384849 | Cytotoxicity against human IGROV1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360963 | Inhibition of Tel-fused FLT1 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384679 | Cytotoxicity against human HPAC cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383599 | Cytotoxicity against human BT-B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654029 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser935 expressed in HEK293 cells at 0.1 to 0.3 uM after 90 mins by immunoblot analysis relative to LRRK2-IN1 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384897 | Cytotoxicity against human LK2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383903 | Cytotoxicity against human HCC38 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653625 | Inhibition of Aurora A assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID775336 | Binding affinity to human FLT3 | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384156 | Cytotoxicity against human SW837 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383642 | Cytotoxicity against human COLO 679 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383909 | Cytotoxicity against human HCE7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653592 | Inhibition of PKCzeta assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID757925 | Activity at insulin receptor in mouse assessed as effect on plasma glucose utilization up to 100 mg/kg by oral glucose tolerance test | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID384418 | Cytotoxicity against human RT4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384658 | Cytotoxicity against human NCI-H1869 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384866 | Cytotoxicity against human KATO III cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID642892 | Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID654026 | Inhibition of wild-type LRRK2 phosphorylation at Ser910 expressed in HEK293 cells at 0.1 to 0.3 uM after 90 mins by immunoblot analysis relative to LRRK2-IN1 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383092 | Inhibition of PDGFRalpha by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384425 | Cytotoxicity against human LoVo cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384149 | Cytotoxicity against human SW48 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384881 | Cytotoxicity against human KU-19-19 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653828 | Inhibition of MLK3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653429 | Inhibition of MKK6 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384680 | Cytotoxicity against human HRT18 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384903 | Cytotoxicity against human WI-26 VA4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384623 | Cytotoxicity against human MFE280 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654012 | Inhibition of SYK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384167 | Cytotoxicity against human TE7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653841 | Inhibition of p38delta MAPK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653816 | Inhibition of MAPKAP-K3 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360994 | Inhibition of RAS/RAF/MAPK signaling in human Karpas299 cells assessed as ERK phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID360951 | Inhibition of NPM-ALK autophosphorylation in human SUDHL1 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653811 | Inhibition of JNK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383859 | Cytotoxicity against human DMS 273 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653634 | Inhibition of CHK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653838 | Inhibition of OSR1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384880 | Cytotoxicity against human KPL1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653834 | Inhibition of MST4 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384685 | Cytotoxicity against human Hs 683 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361010 | Antilymphomal activity against mouse Ba/F3 NPM-ALK cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 10 mg/kg, po once daily after 2 weeks relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384417 | Cytotoxicity against human RT112/84 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653835 | Inhibition of NEK2a assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384164 | Cytotoxicity against human Takigawa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653409 | Inhibition of IRAK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653583 | Inhibition of PDK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653652 | Inhibition of ERK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383619 | Cytotoxicity against human Calu3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653615 | Inhibition of TrkA assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383893 | Cytotoxicity against human HARA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653440 | Inhibition of NUAK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384868 | Cytotoxicity against human KHM3S cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653627 | Inhibition of BRK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653381 | Inhibition of CLK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653425 | Inhibition of MELK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653648 | Inhibition of EPH-B1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383598 | Cytotoxicity against human BT549 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383924 | Cytotoxicity against human SCCH26 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653857 | Inhibition of PKCgamma assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1070245 | Inhibition of recombinant wild type ALK catalytic domain (1064 to 1427) (unknown origin) expressed in baculovirus expression system using ARDIYRASFFRKGGCAMLPVK as substrate preincubated for 10 mins followed by ATP addition measured after 15 mins by ELISA | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
| Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
AID383573 | Cytotoxicity against human A2780 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383917 | Cytotoxicity against human HeLaS3(sc) cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653822 | Inhibition of MELK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383105 | Inhibition of FLT3 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653202 | Inhibition of wild type LRRK2 phosphorylation at Ser910 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653821 | Inhibition of MEKK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383388 | Cytotoxicity against human 1A6 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654023 | Inhibition of VEGFR assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653813 | Inhibition of Lck assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384138 | Cytotoxicity against human SVts8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383586 | Cytotoxicity against human AZ521 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653604 | Inhibition of SmMLCK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653449 | Inhibition of PAK6 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384848 | Cytotoxicity against human IGR39 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384379 | Cytotoxicity against human OUMS23 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653393 | Inhibition of EPH-B3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384624 | Cytotoxicity against human MFE-296 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID642894 | Cytotoxicity against human Kelly cells expressing ALK F1174L mutant | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653386 | Inhibition of DYRK3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383616 | Cytotoxicity against human CAL62 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384659 | Cytotoxicity against human NCI-H1915 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384902 | Cytotoxicity against human VMRC-RCZ cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360940 | Induction of apoptosis in mouse Ba/F3 NPM-ALK cells at 50 nM after 48 hrs by annexin V assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID1310843 | Protein binding in mouse plasma | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
AID384426 | Cytotoxicity against human LS174T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384414 | Cytotoxicity against human RO82-W-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384205 | Cytotoxicity against human NCI-H727 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384373 | Cytotoxicity against human OAW42 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384127 | Cytotoxicity against human SK-OV3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653858 | Inhibition of PKD1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653389 | Inhibition of EPH-A2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653406 | Inhibition of IKKbeta assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1369791 | Antiproliferative activity against human SH-SY5Y cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID384437 | Cytotoxicity against human MCF7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1191199 | Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383916 | Cytotoxicity against human HeLa S3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653795 | Inhibition of FGF-R1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383913 | Cytotoxicity against human HeLa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653206 | Inhibition of wild type LRRK2 phosphorylation at Ser910 in mouse 3T3 cells after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360941 | Inhibition of NPM-ALK in mouse Ba/F3 NPM-ALK cells at 50 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384888 | Cytotoxicity against human KYSE410 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653843 | Inhibition of PAK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383895 | Cytotoxicity against human HBE4-E6E7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653207 | Inhibition of wild type LRRK2 phosphorylation at Ser935 in mouse 3T3 cells after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384855 | Cytotoxicity against human IPTP/98 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384618 | Cytotoxicity against human MEL-HO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653832 | Inhibition of MSK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1529865 | Inhibition of TYRO3 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors. |
AID384199 | Cytotoxicity against human NCI-H520 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383397 | Cytotoxicity against human 8305C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID642888 | Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID384672 | Cytotoxicity against human HPAF-II cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361002 | Cmax in human Karpas299 cells xenografted SCID beige mouse at 20 mg/kg, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383597 | Cytotoxicity against human BT483 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653639 | Inhibition of CSK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383894 | Cytotoxicity against human HBE135-E6E7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361018 | Inhibition of human Karpas299 cells assessed as reduction in CD30 receptor expression on cell surface after 24 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653597 | Inhibition of PRK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID758042 | Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID383400 | Cytotoxicity against human A2058 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383623 | Cytotoxicity against human CCF-STTG1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383622 | Cytotoxicity against human CaR1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383580 | Cytotoxicity against human ABC-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653614 | Inhibition of TLK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653631 | Inhibition of CAMK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383936 | Cytotoxicity against human SK-HEP-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383897 | Cytotoxicity against human HCC1395 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653236 | Inhibition of ASK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653405 | Inhibition of IGF-1R assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384155 | Cytotoxicity against human SW756 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384906 | Cytotoxicity against human WM 266-4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384905 | Cytotoxicity against human WiDr cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384174 | Cytotoxicity against human UACC812 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360972 | Inhibition of Tel-fused SRC kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384194 | Cytotoxicity against human NCI-H2452 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653585 | Inhibition of PIM1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1369785 | Induction of ALK degradation in human KARPAS299 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID384411 | Cytotoxicity against human RERF-LC-Sq1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384383 | Cytotoxicity against human OVISE cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID654011 | Inhibition of STK33 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384887 | Cytotoxicity against human KYSE30 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383344 | Inhibition of Tie2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383925 | Cytotoxicity against human SCH cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384192 | Cytotoxicity against human NCI-H2405 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384670 | Cytotoxicity against human NCI-H2110 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID654010 | Inhibition of SRPK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384147 | Cytotoxicity against human SW1783 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653815 | Inhibition of MAPKAP-K2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653649 | Inhibition of EPH-B2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383612 | Cytotoxicity against human CAL148 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653380 | Inhibition of CK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360961 | Inhibition of Tel-fused KitQ kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653417 | Inhibition of LKB1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384643 | Cytotoxicity against human NCI-H1563 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383577 | Cytotoxicity against human A427 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383929 | Cytotoxicity against human SHP77 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383899 | Cytotoxicity against human HCC1806 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383614 | Cytotoxicity against human CAL51 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384845 | Cytotoxicity against human HUP-T4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653445 | Inhibition of p38gamma MAPK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID654007 | Inhibition of SGK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383611 | Cytotoxicity against human CAL12T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1369813 | Induction of ALK degradation in human Kelly cells assessed as decrease in ALK phosphorylation at Y1507 at 50 to 250 nM after 16 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). |
AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653617 | Inhibition of TTBK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384445 | Cytotoxicity against human MDA-MB-435S cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653860 | Inhibition of PRAK assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384914 | Cytotoxicity against human ZR-75-30 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653808 | Inhibition of IRR assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384674 | Cytotoxicity against human HLF cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653435 | Inhibition of MSK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384617 | Cytotoxicity against human ME180 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653203 | Inhibition of wild type LRRK2 phosphorylation at Ser935 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID642897 | Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID383872 | Cytotoxicity against human EPLC-272H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383933 | Cytotoxicity against human SK-CO1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653134 | Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383615 | Cytotoxicity against human CAL54 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384689 | Cytotoxicity against human HT 1080 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360946 | Antiproliferative activity against mouse Ba/F3 NPM-ALK cells assessed as luciferase expression after 2 to 3 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383927 | Cytotoxicity against human SEG1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384858 | Cytotoxicity against human J82 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653793 | Inhibition of ERK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383393 | Cytotoxicity against human 639-V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653646 | Inhibition of EPH-A2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384387 | Cytotoxicity against human OVTOKO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384401 | Cytotoxicity against human PC-9 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653421 | Inhibition of MARK2 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653632 | Inhibition of CAMKKb assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384187 | Cytotoxicity against human NCI-H2228 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1562812 | Inhibition of wild type FLT3 (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. |
AID1416439 | Inhibition of phosphorylated FGFR1 (407 to 822 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
AID383876 | Cytotoxicity against human TT2609-C02 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID361011 | Toxicity in mouse Ba/F3 NPM-ALK cells xenografted in SCID beige mouse assessed as reduction in spleen weight at 10 mg/kg, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653193 | Inhibition of LRRK2 G2019S mutant phosphorylation at Ser935 expressed in HEK293 cells after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1416443 | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C552A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
AID653243 | Inhibition of CAMK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384180 | Cytotoxicity against human VMRC-LCP cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID360993 | Inhibition of STAT3 in mouse Ba/F3 NPM-ALK cells at 50 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653624 | Inhibition of ASK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384406 | Cytotoxicity against human RERF-GC-1B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384655 | Cytotoxicity against human NCI-H1781 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384863 | Cytotoxicity against human JR 019 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383645 | Cytotoxicity against human COLO 699 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384403 | Cytotoxicity against human PLC/PRF/5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360942 | Inhibition of STAT3 in human Karpas299 cells at 50 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383911 | Cytotoxicity against human HCT8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384185 | Cytotoxicity against human NCI-H2172 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384864 | Cytotoxicity against human JR 029 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653248 | Inhibition of CK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383871 | Cytotoxicity against human EJ138 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653595 | Inhibition of PLK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383931 | Cytotoxicity against human SISO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384668 | Cytotoxicity against human NCI-H2085 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384171 | Cytotoxicity against human U138 MG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384886 | Cytotoxicity against human KYSE270 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383574 | Cytotoxicity against human A373-C6 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653823 | Inhibition of MINK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384642 | Cytotoxicity against human NCI-H1437 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384907 | Cytotoxicity against human WM 1552C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384440 | Cytotoxicity against human MDA-H2774 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653200 | Inhibition of LRRK2 A2016T mutant phosphorylation at Ser910 expressed in HEK293 cells at 1 to 3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384852 | Cytotoxicity against human IM-95m cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384635 | Cytotoxicity against human MS751 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653201 | Inhibition of LRRK2 A2016T mutant phosphorylation at Ser935 expressed in HEK293 cells at 1 to 3 uM after 90 mins by immunoblot analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383589 | Cytotoxicity against human BEAS-2B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383581 | Cytotoxicity against human ACHN cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384396 | Cytotoxicity against human PA-TU-8988S cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653629 | Inhibition of BRSK2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653223 | Inhibition of LRRK2 phosphorylation at Ser935 in C57BL/6 mouse spleen at 50 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384432 | Cytotoxicity against human LU99C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384436 | Cytotoxicity against human MCAS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID1416441 | Inhibition of phosphorylated FGFR3 (411 to 806 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383610 | Cytotoxicity against human CAL120 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1562811 | Inhibition of FES (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. |
AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384910 | Cytotoxicity against human WM793b cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653237 | Inhibition of Aurora A assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID1350816 | Inhibition of TEL-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383881 | Cytotoxicity against human G361 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383578 | Cytotoxicity against human A431 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384630 | Cytotoxicity against human MKN7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360959 | Inhibition of Tel-fused PDGFRb kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383390 | Cytotoxicity against human 23132/87 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1372112 | Inhibition of human EGFR del19/T790M/C797S mutant expressed in mouse Ba/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo assay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer. |
AID653218 | Ratio of AUClast in brain to plasma of Swiss albino mouse at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653849 | Inhibition of PIM1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653836 | Inhibition of NEK6 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384386 | Cytotoxicity against human OVSAYO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID361003 | Antilymphomal activity against human Karpas299 cells xenografted in SCID beige mouse assessed as reduction in bioluminescence signal at 1 mg/kg, po once daily after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID383868 | Cytotoxicity against human EFM-192C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653222 | Inhibition of LRRK2 phosphorylation at Ser910 in C57BL/6 mouse spleen at 50 mg/kg, po administered for 8 hrs followed by 2 hrs dosing | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID360957 | Inhibition of Tel-fused EphB4 kinase-mediated mouse BaF3 cell proliferation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384201 | Cytotoxicity against human NCI-H596 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360985 | Inhibition of FKHR phosphorylation in rat H4-2E cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID360996 | Induction of apoptosis in mouse parental Ba/F3 cells at 50 nM after 48 hrs by annexin V assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653856 | Inhibition of PKCzeta assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID642889 | Cytotoxicity against mouse BAF3 cells expressing NPM-ALK after 48 hrs by CellTiter-Glo assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384193 | Cytotoxicity against human NCI-H2444 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384667 | Cytotoxicity against human NCI-H2073 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384892 | Cytotoxicity against human KYSE520 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383084 | Inhibition of Bcr-abl by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID1416444 | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C477A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384904 | Cytotoxicity against human WI-38 VA13 sub 2 RA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653833 | Inhibition of MST2 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384682 | Cytotoxicity against human Hs 417.Lu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653610 | Inhibition of TAO1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383639 | Cytotoxicity against human COLO 206F cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653390 | Inhibition of EPH-A4 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383646 | Cytotoxicity against human COLO 818 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383653 | Cytotoxicity against human Daoy cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383930 | Cytotoxicity against human SiHa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID361000 | Cell cycle arrest in human Karpas299 cells by accumulation in G1 phase at 25 nM after 72 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID653837 | Inhibition of NUAK1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID653606 | Inhibition of SRPK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384653 | Cytotoxicity against human NCI-H1734 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383910 | Cytotoxicity against human HCT116 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653618 | Inhibition of TTK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384369 | Cytotoxicity against human NUGC2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384894 | Cytotoxicity against human LC-1 sq cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383636 | Cytotoxicity against human COLO 853 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384404 | Cytotoxicity against human QGP1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653135 | Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID654024 | Inhibition of YES1 assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID758044 | Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
AID384372 | Cytotoxicity against human OAW28 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653246 | Inhibition of CHK1 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653422 | Inhibition of MARK3 assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383631 | Cytotoxicity against human COLO 201 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384421 | Cytotoxicity against human Saos-2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383883 | Cytotoxicity against human G402 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383914 | Cytotoxicity against human HeLa 229 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID383391 | Cytotoxicity against human 273T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653215 | Clearance in Swiss albino mouse at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID383618 | Cytotoxicity against human Calu1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID653626 | Inhibition of Aurora B assessed as residual activity at 1 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID384374 | Cytotoxicity against human OCUM1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384873 | Cytotoxicity against human KMRM-M1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653212 | AUClast in Swiss albino mouse plasma at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID383861 | Cytotoxicity against human DoTc2 4510 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384408 | Cytotoxicity against human RERF-LC-Ad2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID384859 | Cytotoxicity against human JHH1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID653596 | Inhibition of PRAK assessed as residual activity at 10 uM relative to control | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Characterization of TAE684 as a potent LRRK2 kinase inhibitor. |
AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID360981 | Inhibition of Bmx kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jan-02, Volume: 104, Issue:1
| Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
AID384172 | Cytotoxicity against human U2 OS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
AID384915 | Cytotoxicity against human SK-NEP1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
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. |
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. |
AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4
| Navigating the kinome. |
AID1801919 | Kinase Assay from Article 10.1021/acschembio.5b00940: \\Structural and Functional Analysis of the Allosteric Inhibition of IRE1a with ATP-Competitive Ligands.\\ | 2016 | ACS chemical biology, 08-19, Volume: 11, Issue:8
| Structural and Functional Analysis of the Allosteric Inhibition of IRE1α with ATP-Competitive Ligands. |
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. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 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. |
AID1345550 | Human ALK receptor tyrosine kinase (Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family) | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |