| Assay ID | Title | Year | Journal | Article |
|---|
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531869 | Inhibition of human ROS using KKKSPGEYVNIEFG as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435664 | Binding constant for MYLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1481078 | Inhibition of human MEK1 using ERK2 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID720476 | Millipore: Percentage of residual kinase activity of PRKCB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1365719 | Cytotoxicity against human HepG2 cells at 100 uM after 3 days by CellTiter-Glo luminescent cell viability assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
| The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
| AID720329 | Millipore: Percentage of residual kinase activity of STK11 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% v/v Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720279 | Millipore: Percentage of residual kinase activity of STK33 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1462569 | Induction of apoptosis in human MFE296 cells assessed as early apoptotic cells at 300 nM by 7-AAD/Annexin staining-based assay (Rvb = 1.5 to 2.1%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1365192 | Inhibition of FLT3 (unknown origin) incubated for 10 mins using FAM-labeled peptide and ATP by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
| Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold. |
| AID1350958 | Inhibition of cMET (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1715143 | Inhibition of human TLK1 using Histone H3 as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1732832 | Inhibition of FGFR2 (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1715180 | Inhibition of human RSK1 using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531315 | Inhibition of human EPHB1 assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1680242 | Inhibition of human Trk-A using myelin basic protein as substrate incubated for 40 mins in presence of [gamma33P]ATP by scintillation counting method | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Novel 5,6-disubstituted pyrrolo[2,3-d]pyrimidine derivatives as broad spectrum antiproliferative agents: Synthesis, cell based assays, kinase profile and molecular docking study. |
| AID720448 | Millipore: Percentage of residual kinase activity of PAK4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624705 | Binding constant for MYLK2 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. |
| AID1285477 | Inhibition of Pim1 kinase (unknown origin) using substrate S3 after 50 mins by HTRF assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors. |
| AID1531375 | Inhibition of human KDR assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1736064 | Inhibition of recombinant human PAK4 kinase domain (300 to 591 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition rate using serine/threonine-20 peptide as substrate at 50 uM incubated for 60 mins in presence of ATP by FRET based Z' | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Synthesis, bioconversion, pharmacokinetic and pharmacodynamic evaluation of N-isopropyl-oxy-carbonyloxymethyl prodrugs of CZh-226, a potent and selective PAK4 inhibitor. |
| AID262370 | Inhibition of C-KIT using 1.0 mM ATP | 2006 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
| AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1368675 | Inhibition of human DAPK1 at 10 uM by ADP-Glo kinase assay | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Small molecule inhibitors of anthrax edema factor. |
| AID1531268 | Inhibition of human CDK6/cyclin-D3 assessed as residual activity at 100 uM using RB protein as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID262976 | Inhibition of ERK2 at 10 uM ATP | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
| AID1715249 | Inhibition of human MYO3B using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1758204 | Inhibition of PDGFRA (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins in presence of ATP by caliper mobility shift assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Ring closure strategy leads to potent RIPK3 inhibitors. |
| AID601550 | Cytotoxicity against human HT-29 cells after 48 hrs by SRB assay | 2011 | Journal of natural products, May-27, Volume: 74, Issue:5
| Metachromins U-W: cytotoxic merosesquiterpenoids from an Australian specimen of the sponge Thorecta reticulata. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720303 | Millipore: Percentage of residual kinase activity of INSR at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720254 | Millipore: Percentage of residual kinase activity of RPS6KA2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1157145 | Inhibition of CDK2/cyclin A2 (unknown origin) | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents. |
| AID1183902 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 3 uM after 18 hrs by inverse MTT assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Melleolides induce rapid cell death in human primary monocytes and cancer cells. |
| AID1715198 | Inhibition of human PKG1beta using LRRASLG as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID256674 | Average Binding Constant for PKMYT1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531874 | Inhibition of human SBK1 using LCGRTGRRNSI as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715123 | Inhibition of human ZAP70 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID49344 | Inhibition of rat brain Casein kinase II | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
| AID1247624 | Inhibition of EGFR (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID126618 | Inhibition of MEK1 phosphorylation by activated human recombinant Raf | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). |
| AID1074867 | Induction of apoptosis in human A2780 cells assessed as cholesterol crystal formation after 24 hrs by acridine orange/propidium iodide staining-based fluorescence microscopy | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Membrane damaging activity of a maslinic acid analog. |
| AID1491367 | Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies. |
| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1348850 | Inhibition human recombinant full length His-tagged Plk1 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold. |
| AID262977 | Inhibition of MAPKAP2 at 10 uM ATP | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
| AID1127411 | Cytotoxicity against HEK293 cells after 72 hrs by CellTiterGlo assay | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | 4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies. |
| AID1531568 | Inhibition of human YSK4 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID256608 | Average Binding Constant for MARK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID426692 | Inhibition of CHK1 at 25 nM by alphascreen assay in presence of 0.01% Triton-X100 | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Identification of inhibitors of checkpoint kinase 1 through template screening. |
| AID256656 | Average Binding Constant for p38-alpha; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID720139 | Millipore: Percentage of residual kinase activity of EPHB2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531651 | Inhibition of human CLK4 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1202435 | Inhibition of KIT (unknown origin) at 10 uM after 30 mins by HTRF method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents. |
| AID1715362 | Inhibition of human EPHA8 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531704 | Inhibition of human FYN using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715345 | Inhibition of human FGFR3 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720218 | Millipore: Percentage of residual kinase activity of FRK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID342541 | Inhibition of human ZAP70 | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives. |
| AID1689398 | Antiproliferative activity against human MCF7 cells measured after 48 hrs under normoxic condition by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID1531531 | Inhibition of human STK38 assessed as residual activity at 100 uM using KKRNRRLSVA as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1462586 | Induction of apoptosis in human T47D cells assessed as late apoptotic cells at 100 nM by 7-AAD/Annexin staining-based assay (Rvb = 3 to 13.4%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1531331 | Inhibition of human FGFR2 assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531333 | Inhibition of human FGFR4 assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1466331 | Inhibition of VEGFR-2 (unknown origin) by HTRF method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors. |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID281696 | Induction of apoptosis in Jurkat cells assessed as PARP cleavage at 1 uM after 30 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
| Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group. |
| AID720158 | Millipore: Percentage of residual kinase activity of FER at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1846769 | Inhibition of ALK (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies. |
| AID640589 | Antiproliferative activity against human LoVo cells after 48 to 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity. |
| AID753283 | Inhibition of AKT1 (unknown origin) at 10 uM after 30 mins by fluorescence assay | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological evaluation of N-(4-hydroxy-3-mercaptonaphthalen-1-yl)amides as inhibitors of angiogenesis and tumor growth. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1206448 | Activation of Caspase 3/7 in human U937 cells assessed as cleavage of Ac-DEVD-AFC at 1 uM after 16 hrs by fluorescence assay relative to control | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Removal of Metabolic Liabilities Enables Development of Derivatives of Procaspase-Activating Compound 1 (PAC-1) with Improved Pharmacokinetics. |
| AID1277435 | Induction of apoptosis in mouse B16F10 cells assessed as dead cells at 0.1 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.11%) | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Cytotoxicity and apoptotic activity of novel organobismuth(V) and organoantimony(V) complexes in different cancer cell lines. |
| AID1314089 | Inhibition of recombinant human N-terminal His-tagged GSK-3beta expressed in Escherichia coli using glycogen synthase-2 as substrate and ATP measured after 30 mins by Kinase-Glo luminescent kinase assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3β inhibitors with anti-depressant activity. |
| AID1624699 | Anti-allergic activity in rat RBL2H3 cells assessed as reduction in mouse anti-DNP IgE-induced TNF-alpha level preincubated for 15 mins followed by mouse anti-DNP IgE-stimulation and measured after 3 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
| Bisorbicillinol inhibits Lyn tyrosine kinase for allergic response on RBL-2H3 cells. |
| AID1524570 | Antiproliferative activity against human BJ cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4
| Synthesis and Biological Studies of (+)-Liquiditerpenoic Acid A (Abietopinoic Acid) and Representative Analogues: SAR Studies. |
| AID350283 | Inhibition of MST2 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1236888 | Inhibition of BCR-ABL1 (unknown origin) assessed as ATP remaining by Kinase-Glo luminescent kinase assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR-ABL kinase inhibitors. |
| AID1531629 | Inhibition of human CDK5/p25 using histone H1 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531657 | Inhibition of human DCAMKL1 using KKLNRTLSFAEPG as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1732833 | Inhibition of FGFR3 (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer. |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1715178 | Inhibition of human RSK2 using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531834 | Inhibition of human PKAcb using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID164478 | Inhibition of human neutrophil protein kinase A (PKA) | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. |
| AID1531590 | Inhibition of human Aurora C using [H-LRRASLG] as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720204 | Millipore: Percentage of residual kinase activity of PRKCI at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1715317 | Inhibition of human IKKbeta using KKKKERLLDDRHDSGLDSMKDEE as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID256614 | Average Binding Constant for YES; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1462545 | Induction of apoptosis in human p53-null PC3 cells assessed as early apoptotic cells at 300 nM by 7-AAD/Annexin staining-based assay (Rvb = 0.6 to 1.4%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1466329 | Inhibition of EGFR (unknown origin) by HTRF method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors. |
| AID350256 | Inhibition of CDK2/cyclinA | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1531456 | Inhibition of human PAK5 assessed as residual activity at 100 uM using RRRLSFAEPG as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID590191 | Inhibition of human recombinant IKK-alpha expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
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| AID720169 | Millipore: Percentage of residual kinase activity of CSF1R at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID402479 | Cytotoxicity against mouse L929 cells at 1 uM preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining | 1997 | Journal of natural products, Aug, Volume: 60, Issue:8
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| AID720217 | Millipore: Percentage of residual kinase activity of PKN2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID55504 | Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 in enzymatic assay by measuring phosphorylation of RbING; not tested | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
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| AID720340 | Millipore: Percentage of residual kinase activity of MAPK1 at 1uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1581525 | Antiproliferative activity against human HCT116 cells measured after 72 hrs under CoCl2-induced hypoxic condition by MTT assay | | | |
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| AID1531742 | Inhibition of human KSR2 using KRREILSRRPSYR as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID415619 | Inhibition of CDK6/cyclin D3 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
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| The development of CNS-active LRRK2 inhibitors using property-directed optimisation. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Xylo-C-nucleosides with a pyrrolo[2,1-f][1,2,4]triazin-4-amine heterocyclic base: Synthesis and antiproliferative properties. |
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| Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID389370 | Inhibition of IL2 production in PHA-stimulated human PBMC after 24 hrs by ELISA | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
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| AID1090400 | Phytotoxicity in Phytophthora capsici zoospores suspension infected Capsicum annuum cv. Hanbyul (pepper) at first branch stage pre-exposed to compound spray on stems before fungal infection at 500 ug/mL under greenhouse conditions | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
| Isolation and antifungal and antioomycete activities of staurosporine from Streptomyces roseoflavus strain LS-A24. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID1666228 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell imaging assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Synthesis and Antitumor Activity of C-7-Alkynylated and Arylated Pyrrolotriazine C-Ribonucleosides. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID435934 | Binding constant for PLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
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| AID1350960 | Inhibition of CDK1/cyclin B (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1531281 | Inhibition of human CK1gamma3 assessed as residual activity at 100 uM using KRRRAL[pS]VASLPGL as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531347 | Inhibition of human GRK5 assessed as residual activity at 100 uM using casein as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID262371 | Inhibition of SRC kinase using 1.0 mM ATP | 2006 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID161244 | Inhibition of Platelet-derived growth factor receptor | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
| AID1715387 | Inhibition of human CLK4 using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1581522 | Antiproliferative activity against human PC3 cells measured after 72 hrs under normoxic condition by MTT assay | | | |
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| AID164360 | Inhibition of kinase activity of Raf/MEK/ERK kinase cascade in ELISA | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). |
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| 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. |
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| AID70049 | Inhibition of Epidermal growth factor receptor | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
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| Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
| AID720099 | Millipore: Percentage of residual kinase activity of CAMK2G at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1090411 | Antimicrobial activity against Magnaporthe grisea assessed as growth inhibition incubated for 4 to 7 fays | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
| Isolation and antifungal and antioomycete activities of staurosporine from Streptomyces roseoflavus strain LS-A24. |
| AID720156 | Millipore: Percentage of residual kinase activity of FGFR4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID567888 | Induction of apoptosis in human MCF7 cells expressing estrogen receptor assessed as increase of PARP cleavage at 10'-5 M after 4 hrs by Western blotting | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
| Syntheses, antiproliferative activity and theoretical characterization of acitretin-type retinoids with changes in the lipophilic part. |
| AID1657501 | Antiproliferative activity against human PANC1 cells assessed as inhibition of cell growth | 2020 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 30, Issue:10
| 4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1733107 | Inhibition of CDKL3 (unknown origin) by NanoBRET cellular target engagement assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. |
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| AID1203682 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID1531829 | Inhibition of human PHKgamma2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1531337 | Inhibition of human FLT4 assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531301 | Inhibition of human DYRK1A assessed as residual activity at 100 uM using RRRFRPASPLRGPPK as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1542196 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Pyridine and nitro-phenyl linked 1,3,4-thiadiazoles as MDR-TB inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Synthesis and Antitumor Activity of C-7-Alkynylated and Arylated Pyrrolotriazine C-Ribonucleosides. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1348853 | Selectivity index, ratio of IC50 for human recombinant GST-tagged Plk3 catalytic domain (58 to 340 residues) expressed in baculovirus expression system to IC50 for human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold. |
| AID1531847 | Inhibition of human PKCzeta using ERMRPRKRQGSVRRRV as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1350968 | Inhibition of ERK1 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1572744 | Cytostatic activity against human Z138 cells | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Synthesis and anti-HSV activity of tricyclic penciclovir and hydroxybutylguanine derivatives. |
| AID1300792 | Inhibition of MSK1 (unknown origin) by mobility shift assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
| AID1368678 | Inhibition of human IRAK at 10 uM by ADP-Glo kinase assay | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Small molecule inhibitors of anthrax edema factor. |
| AID1531923 | Inhibition of human ULK2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1808082 | Antiproliferative activity against HEK293 cells assessed as inhibition rate incubated for 72 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| Discovery of Novel Polycyclic Heterocyclic Derivatives from Evodiamine for the Potential Treatment of Triple-Negative Breast Cancer. |
| AID1090404 | Antimicrobial activity against Xanthomonas vesicatoria assessed as growth inhibition incubated for 4 to 7 days | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
| Isolation and antifungal and antioomycete activities of staurosporine from Streptomyces roseoflavus strain LS-A24. |
| AID1531615 | Inhibition of human CDC7/DBF4 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID303314 | Inhibition of TYRO3 at 10 nM | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID595221 | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4
| Maklamicin, an antibacterial polyketide from an endophytic Micromonospora sp. |
| AID720301 | Millipore: Percentage of residual kinase activity of IKBKB at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435930 | Binding constant for PHKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1531814 | Inhibition of human p70S6K using KKRNRTLTK as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1142608 | Inhibition of ALK3 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1704865 | Inhibition of recombinant human N-terminal GST-HIS6 fused RET M918T mutant C-terminal domain (H658 to S1114 residues) expressed in Sf9 insect cells using TRK-C-derived peptide as substrate in presence of [33P]-ATP by filter binding assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant. |
| AID720327 | Millipore: Percentage of residual kinase activity of LIMK1 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1074844 | Induction of apoptosis in human A2780 cells assessed as caspase 3 activity at 1 uM after 12 hrs relative to control | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Membrane damaging activity of a maslinic acid analog. |
| AID1715421 | Inhibition of human CDC7/DBF4 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1354793 | Induction of apoptosis in human SH-SY5Y cells at 1 uM after 6 hrs by Annexin V-FITC/PI staining based flow cytometry | 2018 | Journal of natural products, 06-22, Volume: 81, Issue:6
| Structures and Activities of Tiahuramides A-C, Cyclic Depsipeptides from a Tahitian Collection of the Marine Cyanobacterium Lyngbya majuscula. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531837 | Inhibition of human PKCb1 using Histone H1 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID415622 | Selectivity ratio of IC50 for CDK2/cyclin A to IC50 for human GSK3-beta | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
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| Preussilides A-F, Bicyclic Polyketides from the Endophytic Fungus Preussia similis with Antiproliferative Activity. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID720087 | Millipore: Percentage of residual kinase activity of CSNK2A2 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID350296 | Inhibition of TAK1 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID627290 | Inhibition of RSK2 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID494406 | Inhibition of MAPKAPK2 | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
| Novel 8-arylated purines as inhibitors of glycogen synthase kinase. |
| AID241397 | Inhibition of Protein kinase C epsilon | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
| AID1247629 | Inhibition of FLT3 (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID599231 | Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay | 2011 | Journal of natural products, May-27, Volume: 74, Issue:5
| Cytotoxic and NF-κB inhibitory constituents of the stems of Cratoxylum cochinchinense and their semisynthetic analogues. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1524568 | Antiproliferative activity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4
| Synthesis and Biological Studies of (+)-Liquiditerpenoic Acid A (Abietopinoic Acid) and Representative Analogues: SAR Studies. |
| AID1531743 | Inhibition of human LATS1 using KKRNRRLSVA as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| AID1646264 | Inhibition of PAK4 (unknown origin) by HTRF assay | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
| PB-10, a thiazolo[4,5-d] pyrimidine derivative, targets p21-activated kinase 4 in human colorectal cancer cells. |
| AID1531654 | Inhibition of human CTK using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720027 | Millipore: Percentage of residual kinase activity of NUAK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1269229 | Cytoprotective activity against H2O2-induced apoptosis in human SH-SY5Y cells assessed as dead cells at 100 nM preincubated for 24 hrs followed by H2O2 addition measured after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analys | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| α-Aryl-N-aryl nitrones: Synthesis and screening of a new scaffold for cellular protection against an oxidative toxic stimulus. |
| AID720443 | Millipore: Percentage of residual kinase activity of NLK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531519 | Inhibition of human SNRK assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435520 | Binding constant for CAMK2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID262363 | Inhibition of Akt3 using 10 uM ATP | 2006 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
| AID720171 | Millipore: Percentage of residual kinase activity of FYN at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1715351 | Inhibition of human ERN2 using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID614653 | Inhibition of human N-terminal His-tagged phosphorylated VEGFR2 assessed as dissociation half life after 60 mins by ligand displacement based enzyme-inhibitor dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID1779846 | Inhibition of GSK3beta (unknown origin) assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold. |
| AID1531792 | Inhibition of human MUSK using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1090410 | Antimicrobial activity against Ilyonectria radicicola assessed as growth inhibition incubated for 4 to 7 days | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
| Isolation and antifungal and antioomycete activities of staurosporine from Streptomyces roseoflavus strain LS-A24. |
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| A small molecule-kinase interaction map for clinical kinase inhibitors. |
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| AID688350 | Cytotoxicity against human G361 cells after 72 hrs by Calcein AM assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae. |
| AID720084 | Millipore: Percentage of residual kinase activity of CSNK1D at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1186610 | Inhibition of Aurora B (unknown origin) using HLRRASLG substrate | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435924 | Binding constant for MARK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID725404 | Ratio of IC50 for TNIK-mediated TCF4/beta-casein transcription in human HCT116 cells to IC50 for TNIK (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
| Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors. |
| AID720460 | Millipore: Percentage of residual kinase activity of PDGFRB at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID303323 | Inhibition of Met kinase at 10 nM | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
| AID435161 | Binding constant for FES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1142606 | Inhibition of ALK1 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1252496 | Inhibition of human MEK1 by kinase inhibition assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2. |
| AID256664 | Average Binding Constant for EGFR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID334305 | Inhibition of pig tubulin polymerization at 6 to 32 ug/ml by turbidity assay | | | |
| AID436042 | Binding constant for full-length PHKG1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1350026 | Cytotoxicity against human HCT116 cells by sulforhodamine B assay | 2018 | Journal of natural products, 02-23, Volume: 81, Issue:2
| Cyclizidine-Type Alkaloids from Streptomyces sp. HNA39. |
| AID720214 | Millipore: Percentage of residual kinase activity of MAPKAPK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1287707 | Effect on cell cycle in human SEM cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 45.75%) | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Anti-proliferative evaluation of monoterpene derivatives against leukemia. |
| AID1410108 | Cytotoxicity against human PC3 cells after 72 hrs by SRB assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4
| Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61. |
| AID1666223 | Antiproliferative activity against human Capan1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell imaging assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Synthesis and Antitumor Activity of C-7-Alkynylated and Arylated Pyrrolotriazine C-Ribonucleosides. |
| AID599959 | Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
| Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
| AID1381812 | Induction of apoptosis in human SUP-B15 cells assessed as necrotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 9.2%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID720462 | Millipore: Percentage of residual kinase activity of PDPK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID164979 | In vitro inhibition of [32P] incorporation into histones by rat brain partially purified Protein kinase C in the presence of PMA, [Ca2+] and phosphatidylserine. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
| Substituted 2-(aminomethyl)piperidines: a novel class of selective protein kinase C inhibitors. |
| AID1650885 | Inhibition of PKC in rat RBL2H3 cells assessed as inhibition of ionomycin-stimulated TNFalpha release preincubated for 15 mins followed by ionomycin stimulation and measured after 3 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
| Variegatic acid from the edible mushroom Tylopilus ballouii inhibits TNF-α production and PKCβ1 activity in leukemia cells. |
| AID1531794 | Inhibition of human MYLK4 using KKRPQRRYSNVF as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1383797 | Inhibition of PLK1 (unknown origin) at 10 uM using Ser/Thr-16 peptide substrate after 60 mins by Z'-LYTE assay relative to control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1308983 | Inhibition of TIE2 (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
| AID720471 | Millipore: Percentage of residual kinase activity of AKT3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID256666 | Average Binding Constant for ABL1(Q252H); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID725935 | Ratio of IC50 for human recombinant N-terminal GST-tagged Plk1 in presence of 3.12 mM of ATP to IC50 for human recombinant N-terminal GST-tagged Plk1 in presence of 62.5 uM of ATP | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
| Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton. |
| AID720150 | Millipore: Percentage of residual kinase activity of FGFR1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID740397 | Inhibition of EGFR tyrosine kinase (unknown origin) using poly (Glu,Tyr) as substrate at 0.5 uM after 40 mins by Kinase-Glo Plus luminescence kinase assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Design, synthesis and in vitro anti-proliferative activity of 4,6-quinazolinediamines as potent EGFR-TK inhibitors. |
| AID1706569 | Inhibition of p38beta (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID1722642 | Selective index, difference between deltaTm for CLK3 A319V mutant (unknown origin) expressed in Escherichia coli to deltaTm for recombinant wild type CLK3 (R134 to T484 residues) (unknown origin) expressed in Escherichia coli | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design 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. |
| AID1779110 | Induction of apoptosis in VEGF-stimulated HUVEC cells assessed as increase in cleaved caspase-9 protein expression at 250 nM measured after 48 hrs by western blot analysis | 2021 | Journal of natural products, 06-25, Volume: 84, Issue:6
| Anti-angiogenesis Function of Ononin via Suppressing the MEK/Erk Signaling Pathway. |
| AID284061 | Antitumor activity against human A431 xenograft in BALB/c nude mouse at 1 mg/kg, ip after 10 days relative control | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
| Antitumor studies. Part 1: design, synthesis, antitumor activity, and AutoDock study of 2-deoxo-2-phenyl-5-deazaflavins and 2-deoxo-2-phenylflavin-5-oxides as a new class of antitumor agents. |
| AID729552 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 5 uM by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
| AID1900714 | Inhibition of GSK3-beta (unknown origin) incubated for 60 mins by ATP-Glo luminescent assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID241336 | Inhibition of Protein kinase C delta | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
| AID1394748 | Inhibition of recombinant human PKA expressed in Escherichia coli using Ulight-RRRSLLE as substrate after 10 mins by LANCE method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
| AID1531825 | Inhibition of human PDGFRbeta using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715406 | Inhibition of human CDK5/p25 using histone H1 as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID284068 | Weight change in human A431 xenografted BALB/c nude mouse at 1 mg/kg, po after 18 days | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
| Antitumor studies. Part 1: design, synthesis, antitumor activity, and AutoDock study of 2-deoxo-2-phenyl-5-deazaflavins and 2-deoxo-2-phenylflavin-5-oxides as a new class of antitumor agents. |
| AID1381809 | Induction of apoptosis in human SUP-B15 cells assessed as early apoptotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.1%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1350979 | Inhibition of IR (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID241894 | Inhibition of Vascular endothelial growth factor receptor in P19 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
| AID1531292 | Inhibition of human DAPK2 assessed as residual activity at 100 uM using KKLNRTLSFAEPG as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435403 | Binding constant for EPHB1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID720199 | Millipore: Percentage of residual kinase activity of PRKCZ at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1351023 | Inhibition of LCK (unknown origin) assessed as remaining activity at 3.05 x 10'-10 M after 120 mins in presence of 33P-ATP (Rvb = 89.74%) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1169354 | Cytotoxicity against human BJ cells | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
| Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group. |
| AID256574 | Average Binding Constant for STK3_m; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1715428 | Inhibition of human CAMK2A using KKALRRQETVDAL as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1394681 | Inhibition of recombinant human Aurora-A using Ulight-RRRSLLE as substrate measured after 15 mins by LANCE assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors. |
| AID1531695 | Inhibition of human FGFR2 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1381798 | Induction of apoptosis in human KOPN8 cells assessed as late apoptotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 9.5%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID436044 | Binding constant for PLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1531779 | Inhibition of human MLK3 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID614650 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 assessed as dissociation half life after 60 mins by activity based 100 fold dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID720037 | Millipore: Percentage of residual kinase activity of AURKB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1351021 | Inhibition of LCK (unknown origin) assessed as remaining activity at 4.88 x 10'-9 M after 120 mins in presence of 33P-ATP (Rvb = 89.74%) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID697542 | Inhibition of VEGFR2 after 60 mins by electrophoretic mobility shift assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Predicting new indications for approved drugs using a proteochemometric method. |
| AID1351019 | Inhibition of LCK (unknown origin) assessed as remaining activity at 7.81 x 10'-8 M after 120 mins in presence of 33P-ATP (Rvb = 89.74%) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID720095 | Millipore: Percentage of residual kinase activity of CAMK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531352 | Inhibition of human haspin assessed as residual activity at 100 uM using Histone H3 as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531919 | Inhibition of human TXK using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID219826 | Inhibition of cAMP dependent protein kinase catalytic subunit of bovine heart | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1689468 | Antiproliferative activity against human MCF7 cells measured after 48 hrs under CoCl2-induced hypoxic condition by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
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| AID1715360 | Inhibition of human EPHB4 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
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| AID1715196 | Inhibition of human PKN1 using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1715167 | Inhibition of human SRMS using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531687 | Inhibition of human ERK5 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715349 | Inhibition of human FER using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
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| AID1277438 | Induction of apoptosis in mouse B16F10 cells assessed as early apoptotic cells at 0.1 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.087%) | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Cytotoxicity and apoptotic activity of novel organobismuth(V) and organoantimony(V) complexes in different cancer cell lines. |
| AID1394735 | Inhibition of recombinant human ABL expressed in insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
| AID1727487 | Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Cytotoxic triterpenoid-safirinium conjugates target the endoplasmic reticulum. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| Yeast glycogen synthase kinase-3beta pathway inhibitors from an organic extract of Streptomyces sp. |
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| AID1900709 | Inhibition of equine serum BChE at 50 uM using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
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| AID1531408 | Inhibition of human MKK4 assessed as residual activity at 100 uM using JNK1 as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531595 | Inhibition of human BRAF using MEK1 (K97R) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531516 | Inhibition of human SIK3 assessed as residual activity at 100 uM using AMARAASAAALARRR as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID435180 | Binding constant for MAPKAPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| AID1330920 | Induction of apoptosis in Brugia malayi microfilariae isolated from peritoneal cavity of infected Meriones unguiculatus after 48 hrs by acridine orange/ethidium bromide dual staining based epifluorescence microscopy | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Sulfonamide chalcones: Synthesis and in vitro exploration for therapeutic potential against Brugia malayi. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1246353 | Induction of apoptosis in human triple-negative MDA-MB-231 cells at 2.5 uM after 6 to 48 hrs by microscopic analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
| AID1715388 | Inhibition of human CSK using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Oxidation of the Meroterpenoid (-)-Terreumol C from the Mushroom Tricholoma terreum: Discovery of Cytotoxic Analogues. |
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| AID350259 | Inhibition of c-Met | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
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| AID1502062 | Inhibition of PDGFRbeta (unknown origin) using ATP and enzyme substrate by kinase-glo Plus luminescence kinase assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and structure-activity relationship studies of a focused library of pyrimidine moiety with anti-proliferative and anti-metastasis activities in triple negative breast cancer. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1765289 | Inhibition of human full length GSK3beta expressed in baculovirus in Sf9 insect cells using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate by ADP-Glo kinase assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
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| AID453815 | Antibacterial activity against Bacillus anthracis deltaANR after 14 hrs by microplate alamar blue assay | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| New dermatological agents for the treatment of psoriasis. |
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| AID1531607 | Inhibition of human CAMK1G using KKALRRQETVDAL as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID238873 | Inhibition of [3H]astemizole binding to Potassium channel HERG; Not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1887946 | Inhibition of full length FLAG/HA/Strep-tagged TLK2 (unknown origin) transfected in HEK293T cells at 50 uM using GST-ASF1 as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins in presence of ATP by Western blot an | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis and biological evaluation of bisindole derivatives as anticancer agents against Tousled-like kinases. |
| AID262982 | Inhibition of C-KIT at 1.0 mM ATP | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
| AID127093 | Inhibition of Mitogen-activated protein kinase p38 | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
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| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
| Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID642586 | Inhibition of GSK3-beta by colorimetric analysis | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Design and combinatorial synthesis of a novel kinase-focused library using click chemistry-based fragment assembly. |
| AID1715158 | Inhibition of human STK32B using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1715392 | Inhibition of human CK2A2 using RRRDDDSDDD as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531326 | Inhibition of human ERN2 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715170 | Inhibition of human SIK3 using AMARAASAAALARRR as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1308964 | Inhibition of JAK3 (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
| AID622360 | Antiproliferative activity against human SW1116 cells after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis, biological evaluation and molecular docking studies of 1,3,4-thiadiazole derivatives containing 1,4-benzodioxan as potential antitumor agents. |
| AID1531830 | Inhibition of human PIM1 using KKRNRTLTK as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID775221 | Inhibition of EGFR (unknown origin) at 10 uM after 30 mins by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II. |
| AID1531633 | Inhibition of human CDK7/cyclin-H/MNAT1 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID55358 | Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 in enzymatic assay by measuring phosphorylation of Rb21; not tested | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
| Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531339 | Inhibition of human FRK assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1481079 | Inhibition of human mTOR/FRAP1 using 4EBP1 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID1531767 | Inhibition of human MEKK2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435168 | Binding constant for LTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1704869 | Inhibition of KIF5B-RET fusion protein (unknown origin) by radiometric assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant. |
| AID241300 | Inhibition of Protein kinase C zeta | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
| AID350278 | Inhibition of JAK3 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID435401 | Binding constant for full-length DRAK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1715130 | Inhibition of human ULK1 using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720326 | Millipore: Percentage of residual kinase activity of LIMK1 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1715302 | Inhibition of human KSR2 using KRREILSRRPSYR as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID720024 | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1351005 | Inhibition of c-SRC (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1706568 | Inhibition of p38alpha (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID1531772 | Inhibition of human MKK4 using JNK1 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1350959 | Inhibition of CAMK2b (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID720193 | Millipore: Percentage of residual kinase activity of HCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1308917 | Inhibition of c-Met (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
| AID1381879 | Induction of apoptosis in human KOPN8 cells assessed as effect on Mcl-1 level after 24 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID1063025 | Cytotoxicity against human MCF7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1
| Leonurusoleanolides E-J, minor spirocyclic triterpenoids from Leonurus japonicus fruits. |
| AID1189695 | Inhibition of telomerase in human HepG2 cells at 2 uM after 2 days by TRAP-ELISA method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells. |
| AID623566 | Induction of apoptosis in human HT-29 cells assessed reduction of mitochondrial membrane potential after 2 hrs by using JC1 staining by fluorescence cell-based assay | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10
| Bioassay-guided isolation of constituents of Piper sarmentosum using a mitochondrial transmembrane potential assay. |
| AID1715377 | Inhibition of human DMPK using KKRNRRLSVA as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720374 | Millipore: Percentage of residual kinase activity of STK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1715242 | Inhibition of human NEK8 using casein as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531365 | Inhibition of human IRAK1 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1779845 | Inhibition of GSK3alpha (unknown origin) assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold. |
| AID1531552 | Inhibition of human TSSK3 assessed as residual activity at 100 uM using KKKVSRSGLYRSPSMPENLNRPR as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435826 | Binding constant for full-length PCTK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID764617 | Induction of apoptosis in rat PC12 cells assessed as procaspase-3 activation at 1 uM after 24 hrs by fluorometric assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Synthesis and initial in vitro biological evaluation of two new zinc-chelating compounds: comparison with TPEN and PAC-1. |
| AID1531348 | Inhibition of human GRK6 assessed as residual activity at 100 uM using casein as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1531583 | Inhibition of human ALK5 using casein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531543 | Inhibition of human TIE2 assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1351015 | Inhibition of LCK (unknown origin) assessed as remaining activity at 2 x 10'-5 M after 120 mins in presence of 33P-ATP (Rvb = 89.74%) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1743551 | Inhibition of FLT3 (unknown origin) in presence of ATP | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID1531369 | Inhibition of human JAK1 assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1247616 | Inhibition of ALK (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID1715176 | Inhibition of human SGK1 using KGSGSGRPRTSSFAEG as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID767334 | Inhibition of ABL1 (unknown origin) at 50 uM after 1 hr by luminescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| AID720310 | Millipore: Percentage of residual kinase activity of INSRR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID385591 | Inhibition of human PKCiota | 2007 | The Journal of biological chemistry, Nov-09, Volume: 282, Issue:45
| Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. |
| AID435796 | Binding constant for ERBB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1063042 | Inhibition of PLK1 (unknown origin) | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1
| Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
| AID1531688 | Inhibition of human ERK7 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID303325 | Inhibition of KIT at 10 nM | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
| AID327393 | Induction of cytochrome c release in mitochondrial fraction of human BJ cell expressing TERT, LT, ST and RAS G12V mutant genes at 1 uM | 2007 | Nature, Jun-14, Volume: 447, Issue:7146
| RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels. |
| AID720321 | Millipore: Percentage of residual kinase activity of MAPK9 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531890 | Inhibition of human STK22D using KKKVSRSGLYRSPSMPENLNRPR as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435444 | Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID627129 | Inhibition of CHK1 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID735918 | Inhibition of Raf1 (unknown origin) at 50 uM | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
| Exploration of 1-(3-chloro-4-(4-oxo-4H-chromen-2-yl)phenyl)-3-phenylurea derivatives as selective dual inhibitors of Raf1 and JNK1 kinases for anti-tumor treatment. |
| AID1531400 | Inhibition of human MEK3 assessed as residual activity at 100 uM using p38alpha as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720118 | Millipore: Percentage of residual kinase activity of STK17A at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1381830 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 70.47%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID1090417 | Antimicrobial activity against Colletotrichum orbiculare assessed as growth inhibition incubated for 4 to 7 days | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
| Isolation and antifungal and antioomycete activities of staurosporine from Streptomyces roseoflavus strain LS-A24. |
| AID1381823 | Cell cycle arrest in human KOPN8 cells assessed as accumulation at S phase at 2 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 66.56%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID1671733 | Antiproliferative activity against human SH-SY5Y cells assessed as cell viability at 2 uM after 48 hrs by CellTiter96 AQueous assay relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID350271 | Inhibition of FLT3 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1531754 | Inhibition of human MAK using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531481 | Inhibition of human PKCnu assessed as residual activity at 100 uM using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531564 | Inhibition of human WNK1 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1462544 | Induction of apoptosis in human p53-null PC3 cells assessed as viable cells at 300 nM by 7-AAD/Annexin staining-based assay (Rvb = 96.5 to 98.6%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1462547 | Induction of apoptosis in human p53-null PC3 cells assessed as nuclear debris at 300 nM by 7-AAD/Annexin staining-based assay (Rvb = 0.1 to 0.5%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1715334 | Inhibition of human GRK1 using casein as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID753284 | Inhibition of EGFR (unknown origin) at 10 uM after 30 mins by fluorescence assay | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological evaluation of N-(4-hydroxy-3-mercaptonaphthalen-1-yl)amides as inhibitors of angiogenesis and tumor growth. |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531758 | Inhibition of human MARK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720053 | Millipore: Percentage of residual kinase activity of BRSK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1439517 | Inhibition of Alexa647 tracer binding to full length recombinant human His-tagged CDK8/Cyclin C expressed in baculovirus expression system at 5 uM preincubated for 20 mins followed by tracer addition measured after 60 mins by TR-FRET based Lanthascreen as | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Discovery of novel CDK8 inhibitors using multiple crystal structures in docking-based virtual screening. |
| AID1183912 | Induction of apoptosis in human primary monocytes assessed as apoptotic bodies formation at 3 uM after 3 hrs by light microscopy | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Melleolides induce rapid cell death in human primary monocytes and cancer cells. |
| AID1715209 | Inhibition of human PKCdelta using ERMRPRKRQGSVRRRV as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531507 | Inhibition of human RSK2 assessed as residual activity at 100 uM using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1471754 | Inhibition of recombinant human ALK C1156Y mutant (1093 to 1411 residues) expressed in baculovirus expression system using 5'FAM-KKSRGDYMTMQIG-CONH as substrate preincubated for 15 mins followed by addition of ATP measured after 1 hr by microfluidic mobil | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
| Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| AID1324448 | Inhibition of BRAF (unknown origin) using FAM-labeled peptide as substrate after 1 hr by Lanthascreen assay | | | |
| AID164969 | Inhibition of rat brain Protein kinase C | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531929 | Inhibition of human WNK2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715275 | Inhibition of human MEKK3 using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256602 | Average Binding Constant for EPHA2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
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| AID1610359 | Selectivity index, ratio of IC50 for recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system to IC50 for recombinant full length human His-tagged PLK1 expressed in baculovirus expression system | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID455587 | Displacement of [8-3H]ATP from human recombinant MK2 (36-400) by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
| 2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode. |
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| AID256564 | Average Binding Constant for MAP3K4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
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| AID513248 | Antiapoptotic activity against staurosporine-induced cell death in human HeLa cells assessed as caspase 7 activity at 10 uM after 24 hrs | 2006 | Nature chemical biology, Sep, Volume: 2, Issue:9
| Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. |
| AID720323 | Millipore: Percentage of residual kinase activity of MAPK10 at 10uM relative to control. Control inhibitor: JAK Inhibitor I at 30.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720399 | Millipore: Percentage of residual kinase activity of TEC at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID536057 | Activation of EGF-induced MEK5 activity in HEK293 cells assessed as phosphorylated ERK5 level at 10 uM after 1 hr by Western blotting relative to control | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
| Structure-activity relationships of benzimidazole-based selective inhibitors of the mitogen activated kinase-5 signaling pathway. |
| AID256651 | Average Binding Constant for DAPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
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| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
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| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID436051 | Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID280401 | Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 10 umol/L ATP | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
| Homology modeling of human Fyn kinase structure: discovery of rosmarinic acid as a new Fyn kinase inhibitor and in silico study of its possible binding modes. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1381822 | Cell cycle arrest in human KOPN8 cells assessed as accumulation at G2/M phase at 2 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 9.67%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID457751 | Inhibition of CHK1 by DELFIA assay | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1895102 | Binding affinity to MST4 (unknown origin) assessed as change in melting temperature by thermal shift based DSF assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
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| AID284058 | Weight change in intratumorally dosed BALB/c nude mouse bearing human A431 cells at 1 mg/kg after 17 days | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
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| AID720020 | Millipore: Percentage of residual kinase activity of ALK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID1732379 | Inhibition of p38 alpha (unknown origin) using Ser/Thr 15 as substrate incubated for 1 hr in presence of ATP by Z'-Lyte assay | | | |
| AID1531592 | Inhibition of human BLK using poly[Glu:Tyr](4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1531661 | Inhibition of human DLK using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID241734 | Inhibition of human Protein kinase C beta 1 using [gamma-33P]-ATP | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1543545 | Inhibition of GSK-3beta (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition by caliper assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease. |
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| Synthetic sulfoglycolipids targeting the serine-threonine protein kinase Akt. |
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| AID1247628 | Inhibition of FGFR3 (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID45083 | Inhibition of purified mammalian brain calcium [Ca(2+)]/Calmodulin dependent kinase | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID720398 | Millipore: Percentage of residual kinase activity of TEC at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID1368673 | Inhibition of human CK1g1 at 10 uM by ADP-Glo kinase assay | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Small molecule inhibitors of anthrax edema factor. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720333 | Millipore: Percentage of residual kinase activity of LCK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID1183915 | Induction of apoptosis in human primary monocytes at 3 uM by PE Annexin V and 7-aminoactinomycin staining based flow cytometry | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
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| AID720389 | Millipore: Percentage of residual kinase activity of NEK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531818 | Inhibition of human PAK3 using RRRLSFAEPG as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720266 | Millipore: Percentage of residual kinase activity of SGK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1183892 | Cytotoxicity against human HeLa cells at 0.001 to 1 uM after 24 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Melleolides induce rapid cell death in human primary monocytes and cancer cells. |
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| Bisorbicillinol inhibits Lyn tyrosine kinase for allergic response on RBL-2H3 cells. |
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| AID1300794 | Inhibition of mouse TSSK1 by luminescent ADP-Glo assay kit | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
| AID219830 | Inhibition of Bovine heart cAMP-dependent protein kinase | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
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| AID1899695 | Time dependent inhibition of wild type N-terminal GST tagged BLK (unknown origin) (1 to 505 residues) expressed in sf21 insect cell using TK as substrate in presence of ATP by HTRF assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK). |
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| Synthesis and Biological Studies of (+)-Liquiditerpenoic Acid A (Abietopinoic Acid) and Representative Analogues: SAR Studies. |
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| AID695573 | Antiproliferative activity against human BGC823 cells after 48 hrs by MTT method | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
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| AID1300787 | Inhibition of RSK1 (unknown origin) by Z-LYTE kinase assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
| AID1531628 | Inhibition of human CDK4/cyclin-D3 using RB-CTF as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1612680 | Inhibition of human PKCalpha using ERMRPRKRQGSVRRRV as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone. |
| AID241157 | Inhibition of human Glycogen synthase kinase-3 beta | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
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| AID1878045 | Inhibition of recombinant N-terminal GST/His6-tagged human FLT3 ITD mutant (571 to 993 residues) expressed in insect cells by LanthaScreen assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID262367 | Inhibition of Chk1 using 10 uM ATP | 2006 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Small molecule inhibitors of anthrax edema factor. |
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| AID1203683 | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
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| AID1481081 | Inhibition of human PKCa using histone H1 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1352739 | Inhibition of c-Met (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Identification of novel N |
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| AID1531909 | Inhibition of human TLK2 using casein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1666667 | Inhibition of VEGFR2 in human MCF7 cells by horseradish peroxidase-coupled TMB substrate based ELISA | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5
| VEGFR-2 inhibiting effect and molecular modeling of newly synthesized coumarin derivatives as anti-breast cancer agents. |
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| AID1917243 | Inhibition of CDK2/cyclin E1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
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| AID720108 | Millipore: Percentage of residual kinase activity of DAPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
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| AID1531751 | Inhibition of human LRRK2 using RLGRDKYKTLRQIRQ as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1531235 | Inhibition of human BTK assessed as residual activity at 100 uM using KVEKIGEGTYGVVYK as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID621707 | Binding affinity to TPL2 immobilized on a sensor chip surface by biacore-based competitive binding assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
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| AID720160 | Millipore: Percentage of residual kinase activity of FES at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1531895 | Inhibition of human STK38 using KKRNRRLSVA as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1666666 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 3 days by MTT assay | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5
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| AID720043 | Millipore: Percentage of residual kinase activity of PTK6 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
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| AID1531727 | Inhibition of human IKKepsilon using casein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID720097 | Millipore: Percentage of residual kinase activity of CAMK2B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1531236 | Inhibition of human c-KIT assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1466330 | Inhibition of FLT3 (unknown origin) by HTRF method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
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| AID1531873 | Inhibition of human RSK4 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID303326 | Inhibition of PDGFRalpha at 10 nM | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
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| AID1471758 | Inhibition of recombinant human ALK G1202R mutant (1093 to 1411 residues) expressed in baculovirus expression system using 5'FAM-KKSRGDYMTMQIG-CONH as substrate preincubated for 15 mins followed by addition of ATP measured after 1 hr by microfluidic mobil | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
| Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| AID629275 | Inhibition of FGFR2 | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
| Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
| AID1531689 | Inhibition of human ERN1 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1624702 | Anti-allergic activity in rat RBL2H3 cells assessed as reduction in calcium ionophore-induced TNF-alpha level preincubated for 15 mins followed by calcium ionophore stimulation and measured after 3 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
| Bisorbicillinol inhibits Lyn tyrosine kinase for allergic response on RBL-2H3 cells. |
| AID1846777 | Inhibition of EGFR (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies. |
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| A quantitative analysis of kinase inhibitor selectivity. |
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| Synthesis, molecular modeling and biological evaluation of N-benzylidene-2-((5-(pyridin-4-yl)-1,3,4-oxadiazol-2-yl)thio)acetohydrazide derivatives as potential anticancer agents. |
| AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| AID1762563 | Inhibition of N-terminal GST-fused human recombinant full length ZAP70 (1 to 619 residues) expressed in baculovirus-infected Sf21 cells using FAM-22 peptide as substrate at 1 uM preincubated with enzyme for 10 mins followed by substrate addition for 30 mi | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor. |
| AID720346 | Millipore: Percentage of residual kinase activity of MARK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold. |
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| AID1531474 | Inhibition of human PKCb2 assessed as residual activity at 100 uM using Histone H1 as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID720065 | Millipore: Percentage of residual kinase activity of CDK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1733104 | Inhibition of MLK1 (unknown origin) by NanoBRET cellular target engagement assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. |
| AID1654689 | Induction of apoptosis in human ARN8 cells assessed as increase in YOYO3 positive cells at 1 uM incubated for 48 hrs measured every 2 hrs by YOYO-3 staining based live cell imaging analysis | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability. |
| AID1715407 | Inhibition of human CDK4/cyclin-D3 using RB-CTF as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531560 | Inhibition of human ULK3 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1189697 | Inhibition of telomerase in human HepG2 cells at 4 uM after 1 day by TRAP-ELISA method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells. |
| AID350295 | Inhibition of SYK | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
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| AID1715370 | Inhibition of human EPHA2 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531705 | Inhibition of human GCK using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1417227 | Cytotoxicity against human HeLa cells assessed as cell viability at 1 uM by XTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Development of novel 2,4-bispyridyl thiophene-based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives. |
| AID1704347 | Inhibition of human ERG | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design and synthesis of 1H-indazole-3-carboxamide derivatives as potent and selective PAK1 inhibitors with anti-tumour migration and invasion activities. |
| AID435442 | Binding constant for SYK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID634543 | Competitive inhibition of human CHK2 using ATP as substrate by DELFIA | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
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| AID1156597 | Inhibition of CDK6/cyclin D1 (unknown origin) at 1 uM after 20 to 30 mins by scintillation counting analysis relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and antitumor activity of pyrido [2,3-d]pyrimidine and pyrido[2,3-d] [1,2,4]triazolo[4,3-a]pyrimidine derivatives that induce apoptosis through G1 cell-cycle arrest. |
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| AID1715383 | Inhibition of human DCAMKL2 using KKLNRTLSFAEPG as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID426699 | Inhibition of CDK1 assessed as Rb (ser780) biotinylated peptide phosphorylation by DELFIA assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Identification of inhibitors of checkpoint kinase 1 through template screening. |
| AID1531887 | Inhibition of human SSTK using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1381887 | Inhibition of RNA polymerase 2 C-terminal domain phosphorylation at Ser2 residue in human KOPN8 cells after 3 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID1246321 | Cell cycle arrest in human triple-negative MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 12 hrs by propidium iodide staining-based flow cytometry (Rvb = 48.36%) | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
| AID415613 | Inhibition of CDK1/Cyclin B | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
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| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720213 | Millipore: Percentage of residual kinase activity of PRKG1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID720098 | Millipore: Percentage of residual kinase activity of CAMK2B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531650 | Inhibition of human CLK3 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1247623 | Inhibition of CDK2/cyclin E (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1887905 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Positioning of an unprecedented 1,5-oxaza spiroquinone scaffold into SMYD2 inhibitors in epigenetic space. |
| AID1532741 | Induction of apoptosis in human MCF10A cells assessed as necrotic cells at 1 uM after 12 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry method (Rvb = 0.57%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and evaluation of chalcone analogues containing a 4-oxoquinazolin-2-yl group as potential anti-tumor agents. |
| AID256599 | Average Binding Constant for TTK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
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| AID720432 | Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: PI-103 at 30.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531785 | Inhibition of human MSK1 using GRPRTSSFAEG as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID45092 | Inhibition of human adenocarcinoma cell line Caco-2 proliferation (Not tested) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). |
| AID720151 | Millipore: Percentage of residual kinase activity of FGFR2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1189699 | Inhibition of telomerase in human HepG2 cells at 4 uM after 3 days by TRAP-ELISA method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells. |
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| AID611838 | Inhibition of VEGFR-1 at 50 uM after 1 hrs by luminescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
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| AID1531717 | Inhibition of human HCK using KVEKIGEGTYGVVYK as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID415626 | Selectivity ratio of IC50 for CDK5/P35 to IC50 for human GSK3-beta | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
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| AID1689701 | Induction of apoptosis in human RPMI-8226 cells assessed as BAX level incubated for 24 hrs by ELISA (Rvb = 56 +/- 1.31 pg/ml) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | 1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226. |
| AID435196 | Binding constant for full-length SRPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID498727 | Inhibition of wild type cSrc | 2009 | Nature chemical biology, Jun, Volume: 5, Issue:6
| A new screening assay for allosteric inhibitors of cSrc. |
| AID1298808 | Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation at 10 uM pre-incubated before substrate addition and measured after 60 mins by LANCE detection method | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors. |
| AID1531756 | Inhibition of human MAPKAPK3 using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715191 | Inhibition of human PLK3 using casein as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| 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. |
| AID1715318 | Inhibition of human IKKalpha using KKKKERLLDDRHDSGLDSMKDEE as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720086 | Millipore: Percentage of residual kinase activity of CSNK2A1 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720412 | Millipore: Percentage of residual kinase activity of VRK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID303324 | Inhibition of FLT3 | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
| AID1356601 | Inhibition of GST-tagged human CDK8/CycC (04 to 109 residues) using kinase tracer 236 probe incubated for 60 mins by TR-FRET assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. |
| AID1536864 | Inhibition of kinase tracer 236 binding to recombinant full length His-tagged human CDK8/CycC expressed in baculovirus expression system at 10 uM preincubated for 20 mins followed by tracer addition and measured after 2 hrs by FRET-based LanthaScreen Eu k | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
| Shape-based virtual screen for the discovery of novel CDK8 inhibitor chemotypes. |
| AID415641 | Inhibition of ERK1 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720390 | Millipore: Percentage of residual kinase activity of NEK3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID745526 | Inhibition of CDK3/Cyclin E (unknown origin)-mediated phosphorylation of peptide substrate incubated for 15 mins prior to substrate addition measured after 90 mins by P33-radiolabeled assay | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
| Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases. |
| AID1531638 | Inhibition of human CHK2 using KKKVSRSGLYRSPSMPENLNRPR as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID55537 | Inhibitory activity against Plasmodium falciparum cyclin dependent protein kinase, Pfmrk | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
| Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1394742 | Inhibition of recombinant human Flt1 expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 15 mins by LANCE method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
| AID1491366 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies. |
| AID256667 | Average Binding Constant for ABL1(E255K); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256658 | Average Binding Constant for p38-beta; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1067087 | Inhibition of PTK6 (unknown origin) phosphorylation using Z'-LYTE-Tyr 1 peptide substrate after 1 hr by fluorescence assay | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Optimization, pharmacophore modeling and 3D-QSAR studies of sipholanes as breast cancer migration and proliferation inhibitors. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID256569 | Average Binding Constant for PAK7/PAK5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1531211 | Inhibition of human AKT1 assessed as residual activity at 100 uM using KGSGSGRPRTSSFAEG as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531616 | Inhibition of human CDK17/Cyclin-A using Histone H1 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1704683 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs under chemically-induced hypoxic condition by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | 3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies. |
| AID1531762 | Inhibition of human MEK1 using ERK2 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID241562 | Inhibition of Epidermal growth factor receptor in P19 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
| AID1350966 | Inhibition of EPHA3 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1715182 | Inhibition of human RON using KKSRGDYMTMQIG as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720387 | Millipore: Percentage of residual kinase activity of NEK11 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1462539 | Induction of apoptosis in human MCF7 cells assessed as nuclear debris at 100 nM by 7-AAD/Annexin staining-based assay (Rvb = 0.2 to 3%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1368683 | Inhibition of human PAK1 at 10 uM by ADP-Glo kinase assay | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Small molecule inhibitors of anthrax edema factor. |
| AID1462521 | Induction of apoptosis in human A2780 cells assessed as early apoptotic cells at 300 nM by 7-AAD/Annexin staining-based assay (Rvb = 1.7 to 2.1%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID415620 | Inhibition of CDK9/cyclin T1 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
| AID720309 | Millipore: Percentage of residual kinase activity of IRAK4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID630397 | Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Synthesis, biological evaluation, and molecular docking studies of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan moiety as potential anticancer agents. |
| AID1531614 | Inhibition of human CAMKK2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715197 | Inhibition of human PKG2 using LRRASLG as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720255 | Millipore: Percentage of residual kinase activity of RPS6KA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1484293 | Induction of apoptosis in human PC3 cells assessed as necrotic cells at 10 uM after 16 hrs by F2N12S orange and SYTOX green double staining based flow cytometry (Rvb = 2 to 3%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Structure-activity relationship studies of 1,7-diheteroarylhepta-1,4,6-trien-3-ones with two different terminal rings in prostate epithelial cell models. |
| AID164479 | Inhibition of Protein kinase A | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
| Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID1531360 | Inhibition of human IGF1R assessed as residual activity at 100 uM using KKKSPGEYVNIEFG as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID611839 | Inhibition of VEGFR-2 at 50 uM after 1 hrs by luminescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors. |
| AID1074863 | Induction of apoptosis in human A2780 cells assessed as cell shrinkage at at 1 uM after 24 hrs by acridine orange/propidium iodide staining-based fluorescence microscopy | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Membrane damaging activity of a maslinic acid analog. |
| AID1531398 | Inhibition of human MEK1 assessed as residual activity at 100 uM using ERK2 as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531358 | Inhibition of human HIPK4 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531529 | Inhibition of human STK32C assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531567 | Inhibition of human YES assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1055899 | Cytotoxicity against human HepG2 cells at 10 uM after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Overman rearrangement and Pomeranz-Fritsch reaction for the synthesis of benzoazepinoisoquinolones to discover novel antitumor agents. |
| AID720330 | Millipore: Percentage of residual kinase activity of STK10 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720082 | Millipore: Percentage of residual kinase activity of CSNK1G3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720192 | Millipore: Percentage of residual kinase activity of GSG2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720350 | Millipore: Percentage of residual kinase activity of MELK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720417 | Millipore: Percentage of residual kinase activity of WNK3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1772909 | Inhibition of EGFR (unknown origin) incubated for 40 mins in presence of Mg/ATP mix by [gamma p33]-ATP based scintillation counting method | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720354 | Millipore: Percentage of residual kinase activity of MAP2K6 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4, 1 mg/mL BSA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720281 | Millipore: Percentage of residual kinase activity of PLK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1462530 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells at 1000 nM by 7-AAD/Annexin staining-based assay (Rvb = 1 to 2.1%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1462519 | Induction of apoptosis in human A2780 cells assessed as nuclear debris at 1000 nM by 7-AAD/Annexin staining-based assay (Rvb = 0.3 to 1.1%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1247615 | Inhibition of AKT1 (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID284067 | Antitumor activity against human A431 xenograft in BALB/c nude mouse at 1 mg/kg, po after 18 days relative control | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
| Antitumor studies. Part 1: design, synthesis, antitumor activity, and AutoDock study of 2-deoxo-2-phenyl-5-deazaflavins and 2-deoxo-2-phenylflavin-5-oxides as a new class of antitumor agents. |
| AID1055889 | Cytotoxicity against human LN18 cells at 10 uM after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Overman rearrangement and Pomeranz-Fritsch reaction for the synthesis of benzoazepinoisoquinolones to discover novel antitumor agents. |
| AID155712 | Inhibition of protein kinase C was evaluated as Inhibitory concentration | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. |
| AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1715444 | Inhibition of human AXL using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720173 | Millipore: Percentage of residual kinase activity of GCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1715380 | Inhibition of human DDR2 using KKSRGDYMTMQIG as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID216916 | Inhibition of Vascular endothelial growth factor receptor 2 | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
| AID720126 | Millipore: Percentage of residual kinase activity of EPHA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1410141 | Inhibition of FAK (unknown origin) by Lanthascreen assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4
| Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors. |
| AID721047 | Inhibition of TNIK-mediated TCF4/beta-casein transcription in human HCT116 cells by beta-lactamase reporter gene assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
| Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors. |
| AID720305 | Millipore: Percentage of residual kinase activity of INSR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435297 | Binding constant for MLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID262975 | Inhibition of CDK1 at 10 uM ATP | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
| AID1481070 | Inhibition of human ABL1 using EAIYAAPFAKKK as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
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| AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1462574 | Induction of apoptosis in human MFE296 cells assessed as late apoptotic cells at 100 nM by 7-AAD/Annexin staining-based assay (Rvb = 3.6 to 6.6%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID262374 | Antiproliferative activity against MiaPaCa-2 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
| AID1531412 | Inhibition of human MLCK2 assessed as residual activity at 100 uM using KKLNRTLSFAEPG as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1247618 | Inhibition of BRAF (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
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| AID455585 | Displacement of [8-3H]ATP from human recombinant phospho-MK2 (36-400) by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
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| AID164194 | Inhibition of Protein kinase C zeta | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
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| AID720088 | Millipore: Percentage of residual kinase activity of CSNK2A2 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID165147 | Inhibition Protein kinase C (PKC) | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
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| AID152141 | Inhibitory activity against Plasmodium falciparum W2 | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID720294 | Millipore: Percentage of residual kinase activity of TGFBR1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3β of substituted quinolines. |
| AID1531303 | Inhibition of human DYRK2 assessed as residual activity at 100 uM using RRRFRPASPLRGPPK as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID53178 | Inhibition of Cyclin-dependent kinase 1 | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
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| Leonurusoleanolides E-J, minor spirocyclic triterpenoids from Leonurus japonicus fruits. |
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| AID377264 | Inhibition of PKC | 2000 | Journal of natural products, Sep, Volume: 63, Issue:9
| Bioactive compounds from Psorothamnus junceus. |
| AID406987 | Induction of apoptosis in HDMEC at 2.1 uM after 5 hrs | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
| Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. |
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| AID1631209 | Inhibition of human recombinant JAK3 using Ulight-CAGAGAIETDKEYYTVKD as substrate by LANCE assay | 2016 | ACS medicinal chemistry letters, Oct-13, Volume: 7, Issue:10
| Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1 |
| AID1466332 | Inhibition of KIT (unknown origin) by HTRF method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors. |
| AID1531504 | Inhibition of human RON assessed as residual activity at 100 uM using KKSRGDYMTMQIG as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID670612 | Induction of apoptosis in human HeLa cells assessed as DNA fragmentation at 2 uM after 48 hrs by agarose gel electrophoresis | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells. |
| AID720198 | Millipore: Percentage of residual kinase activity of IGF1R at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1350976 | Inhibition of VEGFR3 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1736661 | Inhibition of Aurora B (unknown origin) incubated for 1 hrs by HTRF assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Design, synthesis, biological evaluation of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives as novel anticancer agents with Aurora kinase inhibition. |
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| C-terminal tetrapeptides inhibit Aβ42-induced neurotoxicity primarily through specific interaction at the N-terminus of Aβ42. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID720439 | Millipore: Percentage of residual kinase activity of NEK6 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1902781 | Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability by MTT assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID720328 | Millipore: Percentage of residual kinase activity of STK11 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% v/v Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID720146 | Millipore: Percentage of residual kinase activity of ERBB4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1531906 | Inhibition of human TGFBR2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
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| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
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| AID1531464 | Inhibition of human PHKgamma1 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID657571 | Inhibition of bovine brain FAK after 20 mins by turbidimetry | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
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| AID280402 | Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 100 umol/L ATP | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
| Homology modeling of human Fyn kinase structure: discovery of rosmarinic acid as a new Fyn kinase inhibitor and in silico study of its possible binding modes. |
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| Small molecule inhibitors of anthrax edema factor. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID629273 | Inhibition of ERK2 | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1538680 | Induction of mitochondrial membrane potential loss in human DU145 cells after 2 hrs by JC1 staining based fluorescence assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6
| Caspase-Dependent Apoptosis in Prostate Cancer Cells and Zebrafish by Corchorusoside C from Streptocaulon juventas. |
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| Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importin α-2 Expression, and Induce Antitumor Effects against Human Glioma. |
| AID262974 | Inhibition of PKCdelta at 10 uM ATP | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1285291 | Inhibition of human recombinant EGFR at 1 uM after 50 mins by microtiter plate based luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Quinoxalinone (Part II). Discovery of (Z)-3-(2-(pyridin-4-yl)vinyl)quinoxalinone derivates as potent VEGFR-2 kinase inhibitors. |
| AID1704868 | Inhibition of human N-terminal GST-HIS6 fused CCDC6-RET fusion protein (Met1 to Ser503 residues) expressed in Sf9 insect cells using TRK-C-derived peptide as substrate in presence of [33P]-ATP by filter binding assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant. |
| AID1531821 | Inhibition of human PAK6 using RRRLSFAEPG as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1385654 | Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2018 | Journal of natural products, 08-24, Volume: 81, Issue:8
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| AID1350986 | Inhibition of MINK1 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1704867 | Inhibition of recombinant human N-terminal GST-HIS6 fused RET V804M mutant C-terminal domain (H658 to S1114 residues) expressed in Sf9 insect cells using TRK-C-derived peptide as substrate in presence of [33P]-ATP by filter binding assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant. |
| AID720231 | Millipore: Percentage of residual kinase activity of PLK3 at 10uM relative to control. Control inhibitor: Wortmannin at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| AID1764190 | Inhibition of DYRK1B (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Synthesis of novel 1H-Pyrazolo[3,4-b]pyridine derivatives as DYRK 1A/1B inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1481072 | Inhibition of human CDK4/cyclinD1 using RB-CTF as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
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| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435805 | Binding constant for MAP4K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID721050 | Inhibition of TNIK (unknown origin) by ADP glo luminescent assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID435528 | Binding constant for IRAK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1090403 | Antioomycete activity against Phytophthora capsici zoospores suspension infected in pepper plants (cv. Hanbyul) at first branch stage pre-exposed to compound spray on stems before fungal infection assessed as reduction in Phyophthora blight disease severi | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
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| Cytotoxic activity of butane type of 1,7-seco-2,7'-cyclolignanes and apoptosis induction by Caspase 9 and 3. |
| AID262373 | Antiproliferative activity against FL5.12-Akt1 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
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| AID1889866 | Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability measured after 48 hrs by colorimetric based MTT assay | | | |
| AID102199 | Antiproliferative activity against human colon cancer cell line (LoVo cells) using MTT assay | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
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| Oxidation of the Meroterpenoid (-)-Terreumol C from the Mushroom Tricholoma terreum: Discovery of Cytotoxic Analogues. |
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| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
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| AID1727475 | Cytotoxicity against human A-375 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Cytotoxic triterpenoid-safirinium conjugates target the endoplasmic reticulum. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1531582 | Inhibition of human ALK4 using casein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1471755 | Inhibition of recombinant human ALK F1174L mutant (1093 to 1411 residues) expressed in baculovirus expression system using 5'FAM-KKSRGDYMTMQIG-CONH as substrate preincubated for 15 mins followed by addition of ATP measured after 1 hr by microfluidic mobil | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
| Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
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| Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. |
| AID1760625 | Cytotoxicity against human TERT-RPE1 cells assessed as inhibition of cell proliferation measured after 72 hrs by real time imaging analysis | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | N-substituted benzimidazole acrylonitriles as in vitro tubulin polymerization inhibitors: Synthesis, biological activity and computational analysis. |
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| AID1356599 | Inhibition of GST-tagged human CDK9/CycT1 (04 to 110 residues) assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pre-incubated for 60 mins by LANCE Ultra assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
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| AID1063049 | Inhibition of aurora-B (unknown origin) | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1715219 | Inhibition of human PHKgamma1 using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1287685 | Induction of apoptosis in human NALM6 cells assessed as necrotic cells at 0.5 uM measured after 24 hrs by annexin V-propidium iodide staining based flow cytometric analysis (Rvb = 0.0%) | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Anti-proliferative evaluation of monoterpene derivatives against leukemia. |
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| AID1368668 | Inhibition of human Aurora A at 10 uM by ADP-Glo kinase assay | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Small molecule inhibitors of anthrax edema factor. |
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| AID611913 | Inhibition of PDGFR-beta at 20 uM after 1 hrs by luminescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
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| Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors. |
| AID720400 | Millipore: Percentage of residual kinase activity of TEK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1287686 | Induction of apoptosis in human NALM6 cells assessed as late apoptotic cells at 0.5 uM measured after 24 hrs by annexin V-propidium iodide staining based flow cytometric analysis (Rvb = 4.3%) | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Anti-proliferative evaluation of monoterpene derivatives against leukemia. |
| AID1531694 | Inhibition of human FGFR1 using KKKSPGEYVNIEFG as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1394738 | Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
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| AID71178 | Inhibition of Extracellular signal-regulated kinase 2 (Erk2) | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
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| AID418378 | Inhibition of Pim1 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
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| AID1612677 | Inhibition of human JNK1 using ATF2 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone. |
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| AID627128 | Inhibition of CHK2 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
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| AID415627 | Selectivity ratio of IC50 for CDK6/cyclin D3 to IC50 for human GSK3-beta | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
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| AID1727479 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Cytotoxic triterpenoid-safirinium conjugates target the endoplasmic reticulum. |
| AID1778250 | Inhibition of human NADPH oxidase 4 by quantitative sandwich enzyme immunoassay technique | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Beyond direct Nrf2 activation; reinvestigating 1,2,4-oxadiazole scaffold as a master key unlocking the antioxidant cellular machinery for cancer therapy. |
| AID1715215 | Inhibition of human PKA using LCGRTGRRNSI as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1715413 | Inhibition of human CDK2/cyclin-A using histone H1 as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531351 | Inhibition of human GSK3B assessed as residual activity at 100 uM using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1359962 | Inhibition of recombinant human Pim1 expressed in bacterial expression system using histone H1 as substrate after 30 mins by ADP-Glo reagent based luminescence assay | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors. |
| AID1760629 | Antiproliferative activity against human DND41 cells assessed as inhibition of cell proliferation measured after 72 hrs by by real time imaging analysis | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | N-substituted benzimidazole acrylonitriles as in vitro tubulin polymerization inhibitors: Synthesis, biological activity and computational analysis. |
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| AID1725214 | Cytotoxicity against hTERT-immortalized human OKF6 cells assessed as small and rounded cell morphology at 8 uM incubated for 24 hrs by trypan blue dye based light inverted microscopic analysis | | | |
| AID1531713 | Inhibition of human GRK7 using casein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1308943 | Inhibition of EPHA1 (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531752 | Inhibition of human LYN using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1865712 | Inhibition of cell migration in HUVEC cells at 10 uM after 8 hrs by wound healing assay | 2021 | RSC medicinal chemistry, Sep-23, Volume: 12, Issue:9
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| AID1308985 | Inhibition of TYK2 (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1760626 | Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell proliferation measured after 72 hrs by by real time imaging analysis | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | N-substituted benzimidazole acrylonitriles as in vitro tubulin polymerization inhibitors: Synthesis, biological activity and computational analysis. |
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| Small molecule inhibitors of anthrax edema factor. |
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| Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. |
| AID1350975 | Inhibition of FLT3 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID720244 | Millipore: Percentage of residual kinase activity of MST1R at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1169352 | Cytotoxicity against human HepG2 cells | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
| Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID720306 | Millipore: Percentage of residual kinase activity of IRAK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID629279 | Inhibition of GSK3-beta | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
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| AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| AID718909 | Inhibition of LCK | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
| Purpuroines A-J, halogenated alkaloids from the sponge Iotrochota purpurea with antibiotic activity and regulation of tyrosine kinases. |
| AID1715175 | Inhibition of human SBK1 using LCGRTGRRNSI as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1689481 | Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs under CoCl2-induced hypoxic condition by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
| AID1732831 | Inhibition of FGFR4 (unknown origin) | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer. |
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| AID256675 | Average Binding Constant for PTK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID1531555 | Inhibition of human TXK assessed as residual activity at 100 uM using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531763 | Inhibition of human MEK2 using ERK2 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720275 | Millipore: Percentage of residual kinase activity of SRPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
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| AID1055892 | Cytotoxicity against human PC3 cells at 10 uM after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Overman rearrangement and Pomeranz-Fritsch reaction for the synthesis of benzoazepinoisoquinolones to discover novel antitumor agents. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Melleolides induce rapid cell death in human primary monocytes and cancer cells. |
| AID590190 | Inhibition of human recombinant IKK-beta expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
| Structure-based design and biological profile of (E)-N-(4-Nitrobenzylidene)-2-naphthohydrazide, a novel small molecule inhibitor of IκB kinase-β. |
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| AID1762565 | Inhibition of N-terminal GST-fused human recombinant full length SYK (1 to 635 residues) expressed in baculovirus-infected Sf21 cells using FAM-22 peptide as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 mins in pres | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor. |
| AID427624 | Inhibition of recombinant ERK1 expressed in Escherichia coli | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
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| AID1650882 | Inhibition of PKC in rat RBL2H3 cells assessed as inhibition of mouse anti-DNP IgE-stimulated beta-hexosaminidase release preincubated for 15 mins followed by mouse anti-DNP IgE stimulation and measured after 3 hrs by 4-nitropheny1-2-acetamide-2-deoxy-bet | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
| Variegatic acid from the edible mushroom Tylopilus ballouii inhibits TNF-α production and PKCβ1 activity in leukemia cells. |
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| AID1612684 | Inhibition of human JNK2 using ATF2 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone. |
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| AID1612689 | Inhibition of human STK25 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone. |
| AID720111 | Millipore: Percentage of residual kinase activity of DCLK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720434 | Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720284 | Millipore: Percentage of residual kinase activity of MAP3K7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID1531697 | Inhibition of human FGFR4 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1287713 | Induction of apoptosis in human SEM cells assessed as necrotic cells at 1 uM measured after 24 hrs by annexin V-propidium iodide staining based flow cytometric analysis (Rvb = 0.0%) | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Anti-proliferative evaluation of monoterpene derivatives against leukemia. |
| AID1531655 | Inhibition of human DAPK1 using KKLNRTLSFAEPG as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720456 | Millipore: Percentage of residual kinase activity of PASK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720427 | Millipore: Percentage of residual kinase activity of KIT at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531663 | Inhibition of human DMPK2 using KKRPQRRYSNVF as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1462583 | Induction of apoptosis in human T47D cells assessed as nuclear debris at 300 nM by 7-AAD/Annexin staining-based assay (Rvb = 0.2 to 7.7%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID720318 | Millipore: Percentage of residual kinase activity of MAPK8 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ? -mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1055893 | Cytotoxicity against human NCI-H1115 cells at 10 uM after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Overman rearrangement and Pomeranz-Fritsch reaction for the synthesis of benzoazepinoisoquinolones to discover novel antitumor agents. |
| AID720102 | Millipore: Percentage of residual kinase activity of CAMK2D at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1531899 | Inhibition of human TAK1 using casein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720277 | Millipore: Percentage of residual kinase activity of SRPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720036 | Millipore: Percentage of residual kinase activity of AURKA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435640 | Inhibition of wild-type CK2 holoenzyme | 2003 | The Biochemical journal, Sep-15, Volume: 374, Issue:Pt 3
| Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). |
| AID1410110 | Inhibition of ROCK2 (unknown origin) by HTRF assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4
| Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61. |
| AID1531605 | Inhibition of human CAMK1B using KKALRRQETVDAL as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1423195 | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability at 5 uM after 24 hrs by cellTiter-Glo reagent based assay | 2018 | Journal of natural products, 11-26, Volume: 81, Issue:11
| Azaphilone Derivatives from the Fungus Coniella fragariae Inhibit NF-κB Activation and Reduce Tumor Cell Migration. |
| AID720197 | Millipore: Percentage of residual kinase activity of IGF1R at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID720083 | Millipore: Percentage of residual kinase activity of CSNK1D at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID688347 | Cytotoxicity against human K562 cells after 72 hrs by Calcein AM assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae. |
| AID720421 | Millipore: Percentage of residual kinase activity of ZAP70 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID1426965 | Inhibition of recombinant human His-tagged HER2 cytoplasmic domain (676 to 1255 residues) expressed in baculovirus expression system using Poly (Glu, Tyr) as substrate after 40 mins in presence of ATP by luminescence assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs. |
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| AID1277436 | Induction of apoptosis in mouse B16F10 cells assessed as late apoptotic cells at 0.1 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.450%) | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Cytotoxicity and apoptotic activity of novel organobismuth(V) and organoantimony(V) complexes in different cancer cell lines. |
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| AID1531559 | Inhibition of human ULK2 assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720116 | Millipore: Percentage of residual kinase activity of DMPK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720459 | Millipore: Percentage of residual kinase activity of PDGFRA at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531839 | Inhibition of human PKCdelta using ERMRPRKRQGSVRRRV as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720183 | Millipore: Percentage of residual kinase activity of GSK3B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1738913 | Cytotoxicity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Synthesis of some steroidal mitocans of nanomolar cytotoxicity acting by apoptosis. |
| AID611845 | Inhibition of EGFR at 20 uM after 1 hrs by luminescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors. |
| AID1531630 | Inhibition of human CDK5/p35 using histone H1 as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID225703 | Inhibition of myosin light chain kinase (MLCK) from turkey gizzard | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
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| AID720165 | Millipore: Percentage of residual kinase activity of FLT3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID415638 | Inhibition of AKT3 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1059944 | Inhibition of recombinant PKCE (unknown origin) expressed in baculovirus expression system | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors. |
| AID1623696 | Induction of apoptosis in human SUP-B15 cells assessed as late apoptotic cells level at 2 uM after 24 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 83%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
| AID1706573 | Inhibition of STK10 (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID1381800 | Induction of apoptosis in human KOPN8 cells assessed as necrotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.2%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID1531540 | Inhibition of human TEC assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID163341 | Inhibition of Protein kinase C beta 2 | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
| AID1090409 | Antimicrobial activity against Candida albicans assessed as growth inhibition incubated for 4 to 7 fays | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID162839 | Inhibition of Protein kinase C alpha | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
| Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. |
| AID1360784 | Inhibition of human FLT3 ITD-W51 mutant by Hotspot assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID1504786 | Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Platanic acid: A new scaffold for the synthesis of cytotoxic agents. |
| AID1715412 | Inhibition of human CDK2/cyclin-A1 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| 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. |
| AID1203681 | Cytotoxicity against human PC3 cells after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Design and Synthesis of Antitumor Heck-Coupled Sclareol Analogues: Modulation of BH3 Family Members by SS-12 in Autophagy and Apoptotic Cell Death. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435408 | Binding constant for INSR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436021 | Binding constant for LATS2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1244337 | Inhibition of human KDR using and Ulight-CAGAGAIETDKEYYTVKD as substrate after 1 hr by FRET assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | 4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model. |
| AID1383798 | Inhibition of PLK1 (unknown origin) at 1 uM using Ser/Thr-16 peptide substrate after 60 mins by Z'-LYTE assay relative to control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups. |
| AID1504787 | Cytotoxicity against human A549 cells after 96 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Platanic acid: A new scaffold for the synthesis of cytotoxic agents. |
| AID720201 | Millipore: Percentage of residual kinase activity of PRKCH at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1715319 | Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1763643 | Cytotoxicity against human T47D cells assessed as reduction in cell viability after 3 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Novel 4-(piperazin-1-yl)quinolin-2(1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition. |
| AID1462575 | Induction of apoptosis in human MFE296 cells assessed as nuclear debris at 100 nM by 7-AAD/Annexin staining-based assay (Rvb = 0.4 to 0.8%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1532742 | Induction of apoptosis in human MCF10A cells assessed as viable cells at 1 uM after 12 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry method (Rvb = 95.4%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and evaluation of chalcone analogues containing a 4-oxoquinazolin-2-yl group as potential anti-tumor agents. |
| AID1530831 | Inhibition of human full length N-terminal GST tagged CHK1 assessed as residual activity at 3.05 10'-10M (Rvb = 96.94 to 103.06%) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID664019 | Cytotoxicity against human MCF7 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
| Synthesis, biological evaluation and molecular docking studies of novel 2-(1,3,4-oxadiazol-2-ylthio)-1-phenylethanone derivatives. |
| AID1531718 | Inhibition of human HGK using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1726216 | Cytotoxicity against human HMLE cells assessed as reduction in cell metabolic activity after 72 hrs by MTS assay | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
| Staurosporine Analogs Via C-H Borylation. |
| AID1502658 | Antiproliferative activity against human FS4-LTM cells after 24 hrs by WST-1 assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10
| Oxidation of the Meroterpenoid (-)-Terreumol C from the Mushroom Tricholoma terreum: Discovery of Cytotoxic Analogues. |
| AID1715211 | Inhibition of human PKCb1 using Histone H1 as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1715411 | Inhibition of human CDK2/cyclin-E using histone H1 as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1572737 | Cytostatic activity against human hTERT-RPE1 cells | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Synthesis and anti-HSV activity of tricyclic penciclovir and hydroxybutylguanine derivatives. |
| AID1715238 | Inhibition of human NIM1 using KKKVSRSGLYRSPSMPENLNRPR as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID435644 | Binding constant for ABL1(E255K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
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| AID1531409 | Inhibition of human MKK6 assessed as residual activity at 100 uM using p38alpha as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435940 | Binding constant for full-length TSSK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID303315 | Inhibition of CSK at 10 nM | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
| AID435646 | Binding constant for BLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1704684 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs under normaxic condition by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | 3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies. |
| AID720393 | Millipore: Percentage of residual kinase activity of TLK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1059943 | Inhibition of recombinant IKK2 (unknown origin) expressed in baculovirus expression system | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors. |
| AID1068646 | Inhibition of IKKbeta (unknown origin) | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors. |
| AID1560818 | Covalent inhibition of full-length human recombinant BTK assessed as reduction in enzyme recovery at 10-fold molar excess concentration using FITC-Ahx-TSELKKVVALYDYMPMNAND-biotin-NH2 as substrate preincubated for 1 hr followed by enzyme-compound mixture d | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
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| A quantitative analysis of kinase inhibitor selectivity. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720335 | Millipore: Percentage of residual kinase activity of LCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID415615 | Inhibition of CDK3/Cyclin E | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
| AID720261 | Millipore: Percentage of residual kinase activity of MAPK11 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID1531721 | Inhibition of human HIPK3 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531251 | Inhibition of human CDC7/DBF4 assessed as residual activity at 100 uM using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID235786 | Concentration for 50% cell death determined by lysosomal staining in the neutral red viability assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1532740 | Induction of apoptosis in human MCF10A cells assessed as late apoptotic cells at 1 uM after 12 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry method (Rvb = 3.81%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and evaluation of chalcone analogues containing a 4-oxoquinazolin-2-yl group as potential anti-tumor agents. |
| AID720431 | Millipore: Percentage of residual kinase activity of EEF2K at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID126758 | Inhibition of Mitogen activated protein kinase kinase 4 | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID342543 | Suppression of IL2 production in human whole blood after 24 hrs by ELISA | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
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| AID643483 | Competitive inhibition of human Myt1 by TR-FRET assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| In vitro and in silico studies on substrate recognition and acceptance of human PKMYT1, a Cdk1 inhibitory kinase. |
| AID1308960 | Inhibition of IGF-1R (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID241698 | Inhibition of human Protein kinase C gamma using [gamma-33P]-ATP | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. |
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| Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
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| AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
| Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
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| AID262372 | Activity against GSK3 in FL5.12-Akt1 cells | 2006 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
| Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. |
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| AID1531723 | Inhibition of human HPK1 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| A quantitative analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID541031 | Induction of apoptosis in bovine BL3 cells assessed as necrotic after 24 hrs by annexin V/propidium iodide staining-based FACS analysis | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Theileria apicoplast as a target for chemotherapy. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1664190 | Inhibition of HER4 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assay | | | |
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| AID1733105 | Inhibition of MLK2 (unknown origin) by NanoBRET cellular target engagement assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. |
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| A quantitative analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID337242 | Inhibition of phosphatidylinositol kinase | | | |
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| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
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| Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3. |
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| AID1484290 | Induction of apoptosis in human PC3 cells assessed as necrotic cells at 5 uM after 16 hrs by F2N12S orange and SYTOX green double staining based flow cytometry (Rvb = 2 to 3%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Structure-activity relationship studies of 1,7-diheteroarylhepta-1,4,6-trien-3-ones with two different terminal rings in prostate epithelial cell models. |
| AID541029 | Induction of apoptosis in bovine BL3 cells assessed as viable cells after 24 hrs by annexin V/propidium iodide staining-based FACS analysis | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
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| AID465436 | Inhibition of GSK3-beta assessed as NADH level after 10 mins by pyruvate kinase/lactate dehydrogenase coupled spectrophotometric assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta. |
| AID1538563 | Cell cycle arrest in human KOPN8 cells assessed as increase in accumulation at S phase at 2 uM incubated for 24 hrs by propidium iodide staining based flow cytometric analysis | 2019 | Journal of natural products, 05-24, Volume: 82, Issue:5
| Studies of Jatrogossone A as a Reactive Oxygen Species Inducer in Cancer Cellular Models. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1846766 | Inhibition of BRAF (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies. |
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| AID1715164 | Inhibition of human SSTK using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
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| AID1772937 | Inhibition of BRAF V600E mutant (unknown origin) incubated for 40 mins in presence of Mg/ATP mix by [gamma p33]-ATP based scintillation counting method | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
| AID1438359 | Cytotoxicity against mouse Neuro2a cells assessed as cell viability after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Discovery of 1-(3-(benzyloxy)pyridin-2-yl)-3-(2-(piperazin-1-yl)ethyl)urea: A new modulator for amyloid beta-induced mitochondrial dysfunction. |
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| AID1309007 | Inhibition of PKACalpha (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
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| AID274369 | Inhibition of human recombinant SIRT2 at 50 uM | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
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| Metachromins U-W: cytotoxic merosesquiterpenoids from an Australian specimen of the sponge Thorecta reticulata. |
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| AID1531632 | Inhibition of human CDK6/cyclin-D3 using RB protein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1404897 | Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells at 10 uM using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay relat | | | |
| AID102192 | Inhibition of human adenocarcinoma cell line LoVo proliferation (Not tested) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). |
| AID1360769 | Inhibition of human KDR by Hotspot assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1247620 | Inhibition of c-Kit (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID720249 | Millipore: Percentage of residual kinase activity of TYRO3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1664197 | Inhibition of recombinant human N-terminal His-tagged HER2 (676 to 1255 residues) expressed in baculovirus expression system by competitive binding assay | | | |
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| AID614649 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 after 60 mins by ligand displacement based enzyme-inhibitor dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
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| AID342540 | Inhibition of human Syk | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives. |
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| A small molecule-kinase interaction map for clinical kinase inhibitors. |
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| AID1531805 | Inhibition of human NEK8 using casein as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1063046 | Inhibition of IGF1R (unknown origin) | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1
| Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
| AID303316 | Inhibition of EGFR at 10 nM | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
| AID1351018 | Inhibition of LCK (unknown origin) assessed as remaining activity at 3.13 x 10'-7 M after 120 mins in presence of 33P-ATP (Rvb = 89.74%) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1531488 | Inhibition of human PKN1 assessed as residual activity at 100 uM using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715128 | Inhibition of human ULK3 using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720177 | Millipore: Percentage of residual kinase activity of GRK6 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720241 | Millipore: Percentage of residual kinase activity of ROCK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies. |
| AID1531482 | Inhibition of human PKCtheta assessed as residual activity at 100 uM using Histone H1 as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531720 | Inhibition of human HIPK2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1462543 | Induction of apoptosis in human p53-null PC3 cells assessed as nuclear debris at 1000 nM by 7-AAD/Annexin staining-based assay (Rvb = 0.1 to 0.5%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1531903 | Inhibition of human TBK1 using KRRRAL[pS]VASLPGL as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1298810 | Inhibition of human recombinant JAK1 assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors. |
| AID1308961 | Inhibition of INSR (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
| AID745523 | Inhibition of CDK6/Cyclin D1 (unknown origin)-mediated phosphorylation of peptide substrate incubated for 15 mins prior to substrate addition measured after 90 mins by P33-radiolabeled assay | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
| Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases. |
| AID1715443 | Inhibition of human BLK using poly[Glu:Tyr](4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID435679 | Binding constant for PIM3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531334 | Inhibition of human FGR assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531267 | Inhibition of human CDK6/cyclin-D1 assessed as residual activity at 100 uM using RB protein as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1348851 | Inhibition human recombinant GST-tagged Plk3 catalytic domain (58 to 340 residues) expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold. |
| AID720106 | Millipore: Percentage of residual kinase activity of CAMK1D at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID415643 | Inhibition of IKK-beta | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
| AID720186 | Millipore: Percentage of residual kinase activity of HIPK1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID614651 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 assessed as dissociation half life after 60 mins by ligand displacement based enzyme-inhibitor dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID1055900 | Cytotoxicity against human HT-29 cells at 10 uM after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Overman rearrangement and Pomeranz-Fritsch reaction for the synthesis of benzoazepinoisoquinolones to discover novel antitumor agents. |
| AID1715429 | Inhibition of human CAMK1G using KKALRRQETVDAL as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID256590 | Average Binding Constant for EPHB1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256595 | Average Binding Constant for CLK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1736574 | Cytotoxicity against human T47D cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay | | | |
| AID1715190 | Inhibition of human PLK4 using casein as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1530829 | Inhibition of human full length N-terminal GST tagged CHK1 assessed as residual activity at 4.88 10'-9M (Rvb = 96.94 to 103.06%) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1350981 | Inhibition of JAK3 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
| AID1715309 | Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720338 | Millipore: Percentage of residual kinase activity of MAPK3 at 1uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720093 | Millipore: Percentage of residual kinase activity of CSK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1531336 | Inhibition of human FLT3 assessed as residual activity at 100 uM using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1531636 | Inhibition of human CDK9/cyclin-T2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720142 | Millipore: Percentage of residual kinase activity of EPHB3 at 10uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1202434 | Inhibition of EGFR (unknown origin) at 10 uM after 30 mins by HTRF method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents. |
| AID720295 | Millipore: Percentage of residual kinase activity of TGFBR1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720175 | Millipore: Percentage of residual kinase activity of GRK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID248102 | Tested for TNF-alpha-induced RANTES production in A549 cells using ELISA assay; ND is Not done | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 2: Improvement of in vitro activity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1751468 | Cytotoxicity against human A549 cells assessed as cell viability measured by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Angiokinase inhibition of VEGFR-2, PDGFR and FGFR and cell growth inhibition in lung cancer: Design, synthesis, biological evaluation and molecular docking of novel azaheterocyclic coumarin derivatives. |
| AID720021 | Millipore: Percentage of residual kinase activity of ACVR1B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720311 | Millipore: Percentage of residual kinase activity of INSRR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID303332 | Inhibition of Src at 10 nM | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
| Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
| AID1365190 | Inhibition of c-MET (unknown origin) incubated for 10 mins using FAM-labeled peptide and ATP by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
| Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold. |
| AID1381797 | Induction of apoptosis in human KOPN8 cells assessed as early apoptotic cells at 2 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.1%) | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Novel vitexin-inspired scaffold against leukemia. |
| AID718908 | Inhibition of CDK2 | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
| Purpuroines A-J, halogenated alkaloids from the sponge Iotrochota purpurea with antibiotic activity and regulation of tyrosine kinases. |
| AID720233 | Millipore: Percentage of residual kinase activity of PRKX at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID163379 | Inhibition of Protein kinase C delta | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
| AID1247619 | Inhibition of BRAF V599E mutant (unknown origin) after 40 mins by scintillation counting analysis | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
| AID1710632 | Inhibition of human S6K1 using KKRNRTLTK peptide substrate by radiometric assay | 2020 | RSC medicinal chemistry, May-01, Volume: 11, Issue:5
| Computer-aided discovery of phenylpyrazole based amides as potent S6K1 inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1462580 | Induction of apoptosis in human T47D cells assessed as viable cells at 300 nM by 7-AAD/Annexin staining-based assay (Rvb = 74.5 to 94.5%) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
| AID1066416 | Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | The chemical and biological potential of C ring modified triterpenoids. |
| AID1531298 | Inhibition of human DMPK assessed as residual activity at 100 uM using KKRNRRLSVA as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1715352 | Inhibition of human ERN1 using MBP as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID634542 | Competitive inhibition of human CHK1 using ATP as substrate by DELFIA | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
| AID1715299 | Inhibition of human LATS2 using KKRNRRLSVA as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID256581 | Average Binding Constant for CAMK1G; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1715400 | Inhibition of human CDK9/cyclin-T1 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1142609 | Inhibition of ALK4 (unknown origin) by radioisotopic assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/ |
| AID1481087 | Inhibition of PI3Kalpha (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID242696 | Inhibition of Glycogen synthase kinase-3 beta dependent Tau protein serine-396 phosphorylation in human SY5Y cells; NT= not tested | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
| AID1531485 | Inhibition of human PKG1alpha assessed as residual activity at 100 uM using LRRASLG as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID720211 | Millipore: Percentage of residual kinase activity of PRKG1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720302 | Millipore: Percentage of residual kinase activity of INSR at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID723733 | Stabilization of CDK9/Cyclin T (1 to 330 amino acid residues) (unknown origin) assessed as change in melting temperature at 20 uM by differential scanning fluorimetry assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. |
| AID1715179 | Inhibition of human RSK3 using KKLNRTLSVA as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1715430 | Inhibition of human CAMK1D using KKALRRQETVDAL as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID720334 | Millipore: Percentage of residual kinase activity of LCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID389368 | Inhibition of human Syk expressed in Sf9 cells | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
| Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720450 | Millipore: Percentage of residual kinase activity of PAK7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1771925 | Binding affinity to MERTK (571 to 864 residue) (unknown origin) expressed in Escherichia coli Rosetta cells assessed as change in melting temperature by SYPRO orange dye based DSF assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Design and Development of a Chemical Probe for Pseudokinase Ca |
| AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531478 | Inhibition of human PKCgamma assessed as residual activity at 100 uM using ERMRPRKRQGSVRRRV as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID513191 | Antiapoptotic activity against staurosporine-induced cell death in human H1299 cells assessed as caspase 3 activity at 10 uM after 24 hrs | 2006 | Nature chemical biology, Sep, Volume: 2, Issue:9
| Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. |
| AID1531796 | Inhibition of human MYO3B using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID73318 | Inhibition of Fibroblast growth factor receptor | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
| AID720047 | Millipore: Percentage of residual kinase activity of BLK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1184498 | Inhibition of Aurora A (unknown origin) using [33P]-ATP and 10 uM ATP after 2 hrs | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
| Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors. |
| AID1772910 | Inhibition of ErbB4 (unknown origin) incubated for 40 mins in presence of Mg/ATP mix by [gamma p33]-ATP based scintillation counting method | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
| AID1770396 | Cytotoxicity against human Jurkat cells assessed as inhibition of cell viability measured after 72 hrs by real-time IncuCyte proliferation analysis | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Antibacterial and antitumoral properties of 1,2,3-triazolo fused triterpenes and their mechanism of inhibiting the proliferation of HL-60 cells. |
| AID1778246 | Inhibition of TrxR1 (unknown origin) assessed as reduction in DTNB to TNB by colorimetric assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Beyond direct Nrf2 activation; reinvestigating 1,2,4-oxadiazole scaffold as a master key unlocking the antioxidant cellular machinery for cancer therapy. |
| AID718907 | Inhibition of PLK1 | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
| Purpuroines A-J, halogenated alkaloids from the sponge Iotrochota purpurea with antibiotic activity and regulation of tyrosine kinases. |
| AID1762564 | Inhibition of N-terminal GST-fused human recombinant full length ZAP70 (1 to 619 residues) expressed in baculovirus-infected Sf21 cells using FAM-22 peptide as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 mins in pr | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor. |
| AID256582 | Average Binding Constant for NEK9; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID720076 | Millipore: Percentage of residual kinase activity of CHEK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720188 | Millipore: Percentage of residual kinase activity of HIPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1303870 | Inhibition of cMET (unknown origin) using TK substrate-biotin as substrate preincubated with compound followed by substrate addition for 40 mins measured after 1 hr by HTRF assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synthesis, antitumor evaluation and molecular docking studies of [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives. |
| AID1531601 | Inhibition of human c-MER using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID435687 | Binding constant for PAK7/PAK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
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| AID327394 | Induction of cytochrome c release in cytosolic fraction of human BJ cell expressing TERT, LT, ST and RAS G12V mutant genes at 1 uM | 2007 | Nature, Jun-14, Volume: 447, Issue:7146
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| AID1917242 | Inhibition of CDK1/cyclin B (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
| AID1624698 | Anti-allergic activity in rat RBL2H3 cells assessed as reduction in mouse anti-DNP IgE-induced beta-hexosaminidase release preincubated for 15 mins followed by mouse anti-DNP IgE-stimulation and measured after 3 hrs by p-nitrophenyl-2-acetamide-2-deoxy-be | 2019 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
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| 4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors. |
| AID720297 | Millipore: Percentage of residual kinase activity of IGF1R at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID735917 | Inhibition of ERK2 (unknown origin) at 50 uM | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
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| Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61. |
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| AID1531665 | Inhibition of human DYRK1A using RRRFRPASPLRGPPK as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1765288 | Inhibition of human recombinant full length GSK3beta expressed in baculovirus in Sf9 insect cells using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate at 10 uM by ADP-Glo kinase assay relative to control | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
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| A small molecule-kinase interaction map for clinical kinase inhibitors. |
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| Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors. |
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| Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
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| AID606664 | Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
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| A small molecule-kinase interaction map for clinical kinase inhibitors. |
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| AID1531916 | Inhibition of human TSSK3 using KKKVSRSGLYRSPSMPENLNRPR as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID427622 | Inhibition of recombinant Aurora A expressed in Escherichia coli | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
| Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors. |
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| AID415621 | Selectivity ratio of IC50 for CDK1/cyclin B to IC50 for human GSK3-beta | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. |
| AID629263 | Inhibition of AKT1 | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
| Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
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| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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| Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Synthesis of novel 6-(4-substituted piperazine-1-yl)-9-(β-D-ribofuranosyl)purine derivatives, which lead to senescence-induced cell death in liver cancer cells. |
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| Metachromins U-W: cytotoxic merosesquiterpenoids from an Australian specimen of the sponge Thorecta reticulata. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| PB-10, a thiazolo[4,5-d] pyrimidine derivative, targets p21-activated kinase 4 in human colorectal cancer cells. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1917241 | Inhibition of CDK6/cyclin D1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors. |
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| AID1484298 | Induction of apoptosis in human PC3 cells assessed as apoptotic cells at 30 uM after 16 hrs by F2N12S orange and SYTOX green double staining based flow cytometry (Rvb = 2 to 3%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Structure-activity relationship studies of 1,7-diheteroarylhepta-1,4,6-trien-3-ones with two different terminal rings in prostate epithelial cell models. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| A quantitative analysis of kinase inhibitor selectivity. |
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| AID775218 | Inhibition of AKT (unknown origin) at 10 uM after 30 mins by fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1404898 | Inhibition of recombinant human N-terminal GST-tagged HER2 (679 to 1255 residues) expressed in baculovirus infected Sf9 cells at 10 uM using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay relative to control | | | |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID629396 | Inhibition of LCK | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
| Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1531383 | Inhibition of human LIMK1 assessed as residual activity at 100 uM using cofilin as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1365188 | Inhibition of BRAF (unknown origin) incubated for 10 mins using FAM-labeled peptide and ATP by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1531570 | Inhibition of human ZAP70 assessed as residual activity at 100 uM using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1531432 | Inhibition of human MYO3B assessed as residual activity at 100 uM using MBP as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| AID720369 | Millipore: Percentage of residual kinase activity of RPS6KA4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID720380 | Millipore: Percentage of residual kinase activity of MET at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1779098 | Induction of apoptosis in VEGF-stimulated HUVEC cells assessed as increase in early apoptotic cells at 250 nM measured after 48 hrs by AnnexinV-FITC/PI staining based flow cytometry | 2021 | Journal of natural products, 06-25, Volume: 84, Issue:6
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| AID1680980 | Induction of mitochondrial membrane potential loss in human Jurkat cells at 200 nM after 4 hrs by MitoSense Red/7-AAD. flow cytometric analysis | 2020 | Journal of natural products, 08-28, Volume: 83, Issue:8
| Total Synthesis of Natural Lembehyne C and Investigation of Its Cytotoxic Properties. |
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| AID256637 | Average Binding Constant for JNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors. |
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| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
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| Structure-activity relationships of benzimidazole-based selective inhibitors of the mitogen activated kinase-5 signaling pathway. |
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| Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms. |
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| Bioassay-guided isolation of constituents of Piper sarmentosum using a mitochondrial transmembrane potential assay. |
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| Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. |
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| O-Aryl α,β-d-ribofuranosides: synthesis & highly efficient biocatalytic separation of anomers and evaluation of their Src kinase inhibitory activity. |
| AID385588 | Inhibition of human PKCepsilon type M486A mutant | 2007 | The Journal of biological chemistry, Nov-09, Volume: 282, Issue:45
| Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. |
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| AID720122 | Millipore: Percentage of residual kinase activity of EGFR at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID720425 | Millipore: Percentage of residual kinase activity of RAF1 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1531746 | Inhibition of human LCK2 using MBP as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID629268 | Inhibition of CDK2/Cyclin E | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
| Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
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| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID720482 | Millipore: Percentage of residual kinase activity of PRKCE at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
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| AID1531609 | Inhibition of human CAMK2B using KKALRRQETVDAL as substrate by [gamma-33P]-ATP assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
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| AID1090414 | Antimicrobial activity against Sclerotinia sclerotiorum assessed as growth inhibition incubated for 4 to 7 fays | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
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| AID1189696 | Inhibition of telomerase in human HepG2 cells at 2 uM after 3 days by TRAP-ELISA method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells. |
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| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| AID1308971 | Inhibition of p38alpha (unknown origin) incubated for 1 hr by spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
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| Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID163197 | Inhibition of Protein kinase C beta 1 | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
| AID163880 | Inhibition of Protein kinase C gamma | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. |
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| AID720246 | Millipore: Percentage of residual kinase activity of ROS1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2
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| AID1715326 | Inhibition of human GSK3B using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate by [gamma-33P]-ATP assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1531545 | Inhibition of human TLK2 assessed as residual activity at 100 uM using casein as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID1423824 | Inhibition of recombinant human EGFR T790M/L858R double mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | | | |
| AID1531227 | Inhibition of human AXL assessed as residual activity at 100 uM using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
| AID164627 | Inhibition of Protein kinase A (Histone) (not tested) | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
| Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID435279 | Binding constant for full-length CDK9 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1090407 | Antimicrobial activity against Bacillus subtilis subsp. subtilis assessed as growth inhibition incubated for 4 to 7 days | 2006 | Journal of agricultural and food chemistry, Apr-19, Volume: 54, Issue:8
| Isolation and antifungal and antioomycete activities of staurosporine from Streptomyces roseoflavus strain LS-A24. |
| AID1801940 | GSK-3β activity assay from Article 10.1016/j.bioorg.2016.07.007: \\Synthesis of pyrimidin-4-one-1,2,3-triazole conjugates as glycogen synthase kinase-3u00DF inhibitors with anti-depressant activity.\\ | 2016 | Bioorganic chemistry, 10, Volume: 68 | Synthesis of pyrimidin-4-one-1,2,3-triazole conjugates as glycogen synthase kinase-3β inhibitors with anti-depressant activity. |
| AID1801382 | Kinase Assay from Article 10.1111/cbdd.12546: \\Synthesis and Evaluation of 3-(furo[2,3-b]pyridin-3-yl)-4-(1H-indol-3-yl)-maleimides as Novel GSK-3u00DF Inhibitors and Anti-Ischemic Agents.\\ | 2015 | Chemical biology & drug design, Oct, Volume: 86, Issue:4
| Synthesis and Evaluation of 3-(furo[2,3-b]pyridin-3-yl)-4-(1H-indol-3-yl)-maleimides as Novel GSK-3β Inhibitors and Anti-Ischemic Agents. |
| AID1797134 | Kinase Activity Assay from Article 10.1074/jbc.M512374200: \\Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.\\ | 2006 | The Journal of biological chemistry, Aug-25, Volume: 281, Issue:34
| Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity. |
| AID1795401 | PKC assay from Article 10.1021/jm00079a024: \\Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides.\\ | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
| Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. |
| AID1798514 | PLK Kinase Assay from Article 10.1021/bi7008745: \\Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.\\ | 2007 | Biochemistry, Aug-21, Volume: 46, Issue:33
| Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity. |
| AID1795420 | PKC assay from Article 10.1021/jm00053a003: \\Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction.\\ | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. |
| AID1795948 | CDK Kinase Inhibition Assay from Article 10.1016/s0960-894x(03)00461-x: \\Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.\\ | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
| Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID1799368 | Scintillation Proximity Assay from Article 10.1038/nchembio.87: \\Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility.\\ | 2008 | Nature chemical biology, Jun, Volume: 4, Issue:6
| Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. |
| AID1799403 | Tyrosine Kinase Inhibition Assay from Article 10.1038/nchembio.162: \\A new screening assay for allosteric inhibitors of cSrc.\\ | 2009 | Nature chemical biology, Jun, Volume: 5, Issue:6
| A new screening assay for allosteric inhibitors of cSrc. |
| AID1797337 | PKA/PKC Kinase Assay from Article 10.1016/j.bmcl.2005.12.065: \\Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.\\ | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
| AID1799383 | in vitro Kinase Assay from Article 10.1021/cb9002865: \\In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.\\ | 2010 | ACS chemical biology, Feb-19, Volume: 5, Issue:2
| In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. |
| AID1797336 | Akt Kinase Assay from Article 10.1016/j.bmcl.2005.12.065: \\Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.\\ | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. |
| AID1797592 | CDK Activity Assay. from Article 10.1074/jbc.M201233200: \\Structural basis for Chk1 inhibition by UCN-01.\\ | 2002 | The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
| Structural basis for Chk1 inhibition by UCN-01. |
| AID1797591 | Chk1 Enzymatic Assay from Article 10.1074/jbc.M201233200: \\Structural basis for Chk1 inhibition by UCN-01.\\ | 2002 | The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
| Structural basis for Chk1 inhibition by UCN-01. |
| AID1797654 | cFMs Autophosphorylation Fluorescence Polarization End Point Assay. from Article 10.1074/jbc.M608182200: \\Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies.\\ | 2007 | The Journal of biological chemistry, Feb-09, Volume: 282, Issue:6
| Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies. |
| AID1797593 | CDK4 Activity Assay from Article 10.1074/jbc.M201233200: \\Structural basis for Chk1 inhibition by UCN-01.\\ | 2002 | The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
| Structural basis for Chk1 inhibition by UCN-01. |
| AID1797581 | PDK1 Kinase Activity Assay from Article 10.1042/BJ20031119: \\Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition.\\ | 2003 | The Biochemical journal, Oct-15, Volume: 375, Issue:Pt 2
| Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition. |
| AID1799442 | Inhibition Assay from Article 10.1016/1074-5521(95)90124-8: \\Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.\\ | 1995 | Chemistry & biology, Sep, Volume: 2, Issue:9
| Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol. |
| AID1795421 | PKA assay from Article 10.1021/jm00053a003: \\Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction.\\ | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. |
| AID1797363 | Fluorescence Assays for Determination of Binding Affinity. from Article 10.1016/s1097-2765(05)00089-4: \\Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.\\ | 2000 | Molecular cell, Oct, Volume: 6, Issue:4
| Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine. |
| AID1801812 | Kinase-Glo Assay from Article 10.1111/cbdd.12724: \\Synthesis of Novel Oxazolo[4,5-b]pyridine-2-one based 1,2,3-triazoles as Glycogen Synthase Kinase-3u00DF Inhibitors with Anti-inflammatory Potential.\\ | 2016 | Chemical biology & drug design, 06, Volume: 87, Issue:6
| Synthesis of Novel Oxazolo[4,5-b]pyridine-2-one based 1,2,3-triazoles as Glycogen Synthase Kinase-3β Inhibitors with Anti-inflammatory Potential. |
| AID1796959 | Kinase Assay from Article 10.1074/jbc.M413155200: \\Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002.\\ | 2005 | The Journal of biological chemistry, Apr-08, Volume: 280, Issue:14
| Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002. |
| AID1798742 | Radiometric Kinase Assay from Article 10.1074/jbc.M400031200: \\Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.\\ | 2004 | The Journal of biological chemistry, Apr-30, Volume: 279, Issue:18
| Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors. |
| AID1799260 | In Vitro Protein Kinase Assay from Article 10.1124/mol.107.035832: \\Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.\\ | 2007 | Molecular pharmacology, Oct, Volume: 72, Issue:4
| Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. |
| AID1797135 | Kinase Inhibition Assay from Article 10.1074/jbc.M512374200: \\Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.\\ | 2006 | The Journal of biological chemistry, Aug-25, Volume: 281, Issue:34
| Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity. |
| AID1800263 | c-Src Kinase Inhibitory Activity Assay from Article 10.1016/j.bioorg.2014.02.001: \\Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives.\\ | 2014 | Bioorganic chemistry, Apr, Volume: 53 | Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives. |
| AID1799441 | Inhibition Assay from Article 10.1016/1074-5521(95)90124-8: \\Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.\\ | 1995 | Chemistry & biology, Sep, Volume: 2, Issue:9
| Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2003 | Journal of molecular biology, Oct-17, Volume: 333, Issue:2
| Structural characterization of the GSK-3beta active site using selective and non-selective ATP-mimetic inhibitors. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2003 | Journal of molecular biology, Oct-17, Volume: 333, Issue:2
| Structural characterization of the GSK-3beta active site using selective and non-selective ATP-mimetic inhibitors. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2004 | The Journal of biological chemistry, Dec-31, Volume: 279, Issue:53
| A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2004 | The Journal of biological chemistry, Dec-31, Volume: 279, Issue:53
| A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2004 | The Journal of biological chemistry, Oct-08, Volume: 279, Issue:41
| The three-dimensional structure of the ZAP-70 kinase domain in complex with staurosporine: implications for the design of selective inhibitors. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2004 | The Journal of biological chemistry, Oct-08, Volume: 279, Issue:41
| The three-dimensional structure of the ZAP-70 kinase domain in complex with staurosporine: implications for the design of selective inhibitors. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2005 | The Journal of biological chemistry, Apr-08, Volume: 280, Issue:14
| Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2005 | The Journal of biological chemistry, Apr-08, Volume: 280, Issue:14
| Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002. |
| AID1345403 | Human protein kinase C iota (Iota subfamily) | 2007 | The Journal of biological chemistry, Nov-09, Volume: 282, Issue:45
| Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. |
| AID1345720 | Human mitogen-activated protein kinase kinase 6 (STE7 family) | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
| AID1345465 | Human M4 receptor (Acetylcholine receptors (muscarinic)) | 2000 | Molecular pharmacology, Jul, Volume: 58, Issue:1
| Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site. |
| AID1345708 | Human mitogen-activated protein kinase kinase 4 (STE7 family) | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
| AID1345620 | Human homeodomain interacting protein kinase 1 (HIPK subfamily) | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1345912 | Human serine/threonine kinase 3 (MST subfamily) | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1345365 | Human protein kinase N1 (Protein kinase N (PKN) family) | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1345346 | Human calcium/calmodulin-dependent protein kinase II beta subunit (CAMK2 family) | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1345377 | Human protein kinase, cAMP-dependent, catalytic, beta subunit (Protein kinase A) | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
| The synthesis and evaluation of indolylureas as PKCα inhibitors. |
| AID1345286 | Human M1 receptor (Acetylcholine receptors (muscarinic)) | 2000 | Molecular pharmacology, Jul, Volume: 58, Issue:1
| Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site. |
| AID1345742 | Human phosphorylase kinase catalytic subunit gamma 2 (Phosphorylase kinase (PHK) family) | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1345771 | Human p21 (RAC1) activated kinase 2 (PAKA subfamily) | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1345326 | Human M2 receptor (Acetylcholine receptors (muscarinic)) | 2000 | Molecular pharmacology, Jul, Volume: 58, Issue:1
| Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site. |
| AID1345641 | Human death associated protein kinase 1 (Death-associated kinase (DAPK) family) | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1345878 | Human TRAF2 and NCK interacting kinase (MSN subfamily) | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
| Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 1997 | Structure (London, England : 1993), Dec-15, Volume: 5, Issue:12
| Staurosporine-induced conformational changes of cAMP-dependent protein kinase catalytic subunit explain inhibitory potential. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2006 | Biochemical and biophysical research communications, Aug-04, Volume: 346, Issue:3
| Structure of human Fyn kinase domain complexed with staurosporine. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2006 | Biochemical and biophysical research communications, Aug-04, Volume: 346, Issue:3
| Structure of human Fyn kinase domain complexed with staurosporine. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2006 | Acta biochimica et biophysica Sinica, Jun, Volume: 38, Issue:6
| Crystal structure of the MAP3K TAO2 kinase domain bound by an inhibitor staurosporine. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2006 | Acta biochimica et biophysica Sinica, Jun, Volume: 38, Issue:6
| Crystal structure of the MAP3K TAO2 kinase domain bound by an inhibitor staurosporine. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2004 | The Journal of biological chemistry, Nov-26, Volume: 279, Issue:48
| Catalytic domain crystal structure of protein kinase C-theta (PKCtheta). |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2004 | The Journal of biological chemistry, Nov-26, Volume: 279, Issue:48
| Catalytic domain crystal structure of protein kinase C-theta (PKCtheta). |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2002 | The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
| Structural basis for Chk1 inhibition by UCN-01. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2002 | The Journal of biological chemistry, Nov-29, Volume: 277, Issue:48
| Structural basis for Chk1 inhibition by UCN-01. |
| AID602156 | Novartis GNF Liver Stage Dataset: Malariabox Annotation | 2011 | Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
| Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2007 | Protein science : a publication of the Protein Society, Dec, Volume: 16, Issue:12
| Crystal structures of the N-terminal kinase domain of human RSK1 bound to three different ligands: Implications for the design of RSK1 specific inhibitors. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| Structural basis for the inhibitor recognition of human Lyn kinase domain. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2010 | Biochemistry, Mar-02, Volume: 49, Issue:8
| Biophysical and X-ray crystallographic analysis of Mps1 kinase inhibitor complexes. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |