| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| AID1178744 | Antitumor activity against human HCT116 cells xenografted in BALB/C mouse assessed as reduction in tumor volume at 30 mg/kg, po dosed once daily for 14 days | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents. |
| AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1876143 | Cytotoxicity against HEK293T cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1152723 | Inhibition of human PI3K-beta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1509593 | Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by CCK-8 assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
| Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1389658 | Antiproliferative activity against human SNU638 cells after 72 hrs by sulforhodamine B assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID701557 | Inhibition of PI3Kbeta | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Recent results in protein kinase inhibition for tropical diseases. |
| AID1623553 | Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1427065 | Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2 as substrate after 1 hr by ADP-Glo kinase assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
| AID1245327 | Inhibition of mTORC1 (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1398706 | Inhibition of PI3Kgamma (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1768751 | Antiproliferative activity against human HEL cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition. |
| AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425184 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424931 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1406826 | Inhibition of PI3K-gamma (unknown origin) after 40 mins by Kinase-Glo assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship. |
| AID1568309 | Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID648343 | Growth inhibition of human MDA-MB-231 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID752995 | Toxicity in rag1-deficient mouse xenografted with human U87MG cells assessed as body weight loss at 15 mg/kg, ip qd after 14 days relative to control | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474). |
| AID1303560 | Cytotoxicity against human K562 cells assessed as decrease in cell viability after 24 to 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1871780 | Inhibition of PI3Kalpha (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review. |
| AID1303591 | Potentiation of 0.025 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.005 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424973 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648348 | Growth inhibition of human SNB75 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1600813 | Antiproliferative activity against human Raji cells by MTT assay | | | |
| AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1381741 | Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1321991 | Inhibition of human recombinant PI3KC2alpha using substrate PI incubated for 1 hr by Adapta kinase assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1857287 | Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | | | |
| AID1871784 | Inhibition of mTOR (unknown origin) | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review. |
| AID1396660 | Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors. |
| AID648368 | Growth inhibition of human RXF631L cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1421732 | Inhibition of PI3Kdelta (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors. |
| AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1321996 | Inhibition of human recombinant mTOR using substrate PI incubated for 1 hr by Adapta kinase assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1425066 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1754885 | Inhibition of mTOR (unknown origin) at 0.5 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. |
| AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1398719 | Inhibition of recombinant human full length N-terminal His-tagged PI3K p110delta/p85alpha at 200 nM using lipid substrate after 60 mins by ADP-Glo assay relative to control | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1593871 | AUC (0 to infinity) in C57BL/6J mouse 3 mg/kg, po measured up to 30 hrs by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1706195 | Inhibition of PI3Kalpha (unknown origin) | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1250151 | Cytotoxicity against human Glioma cells (HF2876) after 72 hrs by CelltiterGlo assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. |
| AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648342 | Growth inhibition of human MCF7 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424918 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1568313 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1883103 | Displacement of Alexa Fluor labelled Tracer-314 from human N-terminal GST-tagged mTOR incubated for 1 hr by TR-FRET assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425119 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648501 | Growth inhibition of human MKN28 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1883107 | Binding affinity to human N-terminal GST-tagged mTOR assessed as phosphorylated 4EBP1 by TR-FRET assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID1593869 | Half life in C57BL/6J mouse at 3 mg/kg, po measured up to 30 hrs by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1321992 | Inhibition of human recombinant PI3KC2beta using substrate PI incubated for 1 hr by Adapta kinase assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1421730 | Inhibition of PI3Kbeta (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors. |
| AID1250149 | Cytotoxicity against human Glioma cells (HF2476) after 72 hrs by CelltiterGlo assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. |
| AID1250153 | Cytotoxicity against human Glioma cells (HF3013) after 72 hrs by CelltiterGlo assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. |
| AID701556 | Inhibition of PI3Kdelta | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Recent results in protein kinase inhibition for tropical diseases. |
| AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1593867 | Tmax in C57BL/6J mouse at 3 mg/kg, po measured up to 30 hrs by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1303691 | Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID648341 | Growth inhibition of human HBC5 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1398715 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1424895 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1706196 | Inhibition of PI3Kbeta (unknown origin) | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1706193 | Induction of apoptosis in human Raji cells assessed as late apoptotic cells at 5 uM measured after 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 2.11 %) | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1398720 | Inhibition of recombinant human full length N-terminal His-tagged PI3K p110delta/p85alpha using lipid substrate after 60 mins by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424987 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1433190 | Inhibition of P110gamma/PIK3R5 (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
| AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1398705 | Inhibition of PI3Kbeta (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1593852 | Inhibition of human PI3Kdelta using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1433188 | Inhibition of P110alpha/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
| AID1600815 | Antiproliferative activity against human MCF7 cells by MTT assay | | | |
| AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425167 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1473739 | Inhibition of human MRP2 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. |
| AID1629984 | Inhibition of PI3Kgamma (unknown origin) assessed as reduction in ADP formation using phosphatidyl inositol as substrate after 30 to 60 mins by TR-FRET assay | 2016 | ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
| Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors. |
| AID1152732 | Inhibition of receptor-mediated endocytosis in Trypanosoma brucei brucei Lister 427 assessed as decrease in transferrin uptake at 2 X EC50 after 18 hrs | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1876147 | Inhibition of PI3K alpha (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1629277 | Antiparasitic activity against bloodstream form of Trypanosoma brucei 221 infected in mouse VSMC assessed as parasitic proliferation at 1 uM after 48 hrs by luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19
| Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. |
| AID1303593 | Potentiation of 0.25 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.05 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1250150 | Cytotoxicity against human Glioma cells (HF2790) after 72 hrs by CelltiterGlo assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. |
| AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1685475 | Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream forms after 72 hrs by resazurin dye based fluorescence assay | 2020 | RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
| Structure-property studies of an imidazoquinoline chemotype with antitrypanosomal activity. |
| AID1152724 | Inhibition of human PI3K-gamma assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1876148 | Antiviral activity against LCMV assessed as log reduction in virus progeny at 0.5 to 5 uM | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID648349 | Growth inhibition of human SNB78 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1389656 | Antiproliferative activity against human SKHEP1 cells after 72 hrs by sulforhodamine B assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1509589 | Inhibition of PI3K gamma (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
| Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1152725 | Inhibition of human PI3K-delta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648367 | Growth inhibition of human SKOV3 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425010 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1152722 | Inhibition of human PI3K-alpha assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1568335 | Toxicity in BALB/c mouse xenografted with human HeLa cells assessed as reduction in body weight at 20 mg/kg, ig administered for 30 days | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1768748 | Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition. |
| AID648357 | Growth inhibition of human NCI-H522 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648500 | Growth inhibition of human MKN7 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425042 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425107 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1250152 | Cytotoxicity against human Glioma cells (HF2885) after 72 hrs by CelltiterGlo assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. |
| AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID626744 | Toxicity in PTEN-deficient human U87MG cells xenografted Rag1-/- mouse assessed as body weight loss at 15 mg/kg, ip qd for 10 days | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474). |
| AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID728987 | Inhibition of DNA-PK (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1623566 | Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 24.65%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1300665 | Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs by Z2 coulter counter method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Straightforward synthesis of a novel ring-fused pyrazole-lactam and in vitro cytotoxic activity on cancer cell lines. |
| AID1623562 | Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 1.08%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1623573 | Cell cycle arrest in human Ramos cells assessed as accumulation at apoptotic phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 5.03%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1875977 | Antiviral activity against HIV p24 assessed as extracellular antigen accumulation in primary macrophage at 25 uM | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1424941 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424906 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1421733 | Inhibition of mTORC1 (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors. |
| AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID748656 | Anticancer activity against mouse BA/F3 cells expressing JAK2 V617F mutation allografted in Harlan SCID mouse assessed as increase in lifespan at 45 mg/kg, po by luciferase reporter gene assay relative to control | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Combination Therapy: JAK PI3K/mTOR. A Novel Approach for Cancer Treatment. |
| AID1425212 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1303596 | Potentiation of 7 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 1.4 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1178739 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents. |
| AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1768750 | Antiproliferative activity against human SH-SY5Y assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition. |
| AID1185488 | Cytotoxicity against human PC3 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Click chemistry inspired synthesis and bioevaluation of novel triazolyl derivatives of osthol as potent cytotoxic agents. |
| AID648499 | Growth inhibition of human MKN1 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID648354 | Growth inhibition of human HCT116 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648498 | Growth inhibition of human St-4 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1424975 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424984 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1238956 | Inhibition of PI3Kgamma (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1381748 | Inhibition of PI3K p110delta (unknown origin) using PIP2 as substrate by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1424948 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1300670 | Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 72 hrs by Z2 coulter counter method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Straightforward synthesis of a novel ring-fused pyrazole-lactam and in vitro cytotoxic activity on cancer cell lines. |
| AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424959 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1565368 | Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID767467 | Inhibition of JAK3 (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Selectivity data: assessment, predictions, concordance, and implications. |
| AID1424899 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424914 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1250147 | Cytotoxicity against human Glioma cells (HF2303) after 72 hrs by CelltiterGlo assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. |
| AID1263097 | Cytotoxicity against human PC3 cells after 72 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID1565367 | Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID1424937 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1379446 | Growth inhibition of human U87MG cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1425154 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1396663 | Inhibition of recombinant human PI3K-delta using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors. |
| AID1593851 | Inhibition of human PI3Kdelta using PIP2 as substrate at 100 nM after 1 hr relative to control | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| 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
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1600812 | Antiproliferative activity against human Ramos cells by MTT assay | | | |
| AID1178738 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents. |
| AID1396659 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors. |
| AID1329084 | Inhibition of PI3Kalpha (unknown origin) using diC8 PIP2 as substrate at 0.5 uM after 80 mins by ADP-glo assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID648366 | Growth inhibition of human OVCAR8 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1637614 | Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
| Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors. |
| AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1303589 | Potentiation of 2.5 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.5 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1398713 | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1381745 | Inhibition of PI3K p110alpha (unknown origin) using PIP2 as substrate by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1226264 | Inhibition of PI3Kalpha (unknown origin) using PIP2/PS as substrate after 1 hr by luciferase-based luminescence assay | 2015 | ACS medicinal chemistry letters, Apr-09, Volume: 6, Issue:4
| Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors. |
| AID765569 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and anticancer activity evaluation of a series of [1,2,4]triazolo[1,5-a]pyridinylpyridines in vitro and in vivo. |
| AID1427061 | Inhibition of recombinant full length human N-terminal His6-tagged PI3K p110beta/p85alpha expressed in baculovirus infected Sf21 cells using PIP2 as substrate after 1 hr by ADP-Glo kinase assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
| AID1263098 | Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID1238954 | Inhibition of PI3Kalpha (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID648344 | Growth inhibition of human U251 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1637616 | Inhibition of PI3Kbeta (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay | 2016 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
| Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors. |
| AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1329062 | Inhibition of PI3Kalpha/p85 iSH2 domain (unknown origin) expressed in baculovirus using l-alpha-phosphatidylinositol as substrate after 60 mins by kinase-glo assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1433187 | Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
| AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424894 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424983 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1568315 | Inhibition of recombinant human full length N-terminal GST-tagged PI3Kdelta (1 to 1044 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1565374 | Inhibition of mTOR (unknown origin) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID648363 | Growth inhibition of human OVCAR3 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1245324 | Inhibition of p110beta/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1303585 | Potentiation of 0.025 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.005 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID648503 | Growth inhibition of human MKN74 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648505 | Growth inhibition of human PC3 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID648350 | Growth inhibition of human HCC2998 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1593853 | Inhibition of human PI3Kalpha using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1406827 | Inhibition of PI3K-delta (unknown origin) after 40 mins by Kinase-Glo assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship. |
| AID1629987 | Inhibition of PI3Kdelta (unknown origin) assessed as reduction in ADP formation using phosphatidyl inositol as substrate after 30 to 60 mins by TR-FRET assay | 2016 | ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
| Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors. |
| AID1565369 | Inhibition of PI3Kalpha (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID1490314 | Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4
| Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. |
| AID1424932 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1379444 | Growth inhibition of human MCF7 cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1300675 | Cytotoxicity against human U87MG cells assessed as reduction in cell viability by Z2 coulter counter method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Straightforward synthesis of a novel ring-fused pyrazole-lactam and in vitro cytotoxic activity on cancer cell lines. |
| AID1245326 | Inhibition of p110delta/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1398707 | Inhibition of PI3Kdelta (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1303689 | Potentiation of (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as (-)-lomaiviticin A ED50 at compound to (-)-lomaiviticin A ratio of 200:1 after 48 hrs by cell titer-glo luminescence assay (Rvb = 0.23776 nM) | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1424945 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1593881 | Antiarthritic activity in complete Freund's adjuvant-induced DBA1/J mouse arthritis model assessed as inhibition in clinical arthritis score at 60 mg/kg, po administered for 14 days relative to control | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1629982 | Inhibition of recombinant PI3Kalpha (unknown origin) using phosphatidyl inositol as substrate after 30 to 60 mins in presence of ATP by Kinase Glo luminescence assay | 2016 | ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
| Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors. |
| AID1509588 | Inhibition of PI3K beta (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
| Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1329188 | Selectivity ratio of IC50 for PI3Kdelta (unknown origin) expressed in baculovirus co-expressing p85 to IC50 for PI3Kalpha/p85 iSH2 domain (unknown origin) expressed in baculovirus | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1425095 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648504 | Growth inhibition of human DU145 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID648364 | Growth inhibition of human OVCAR4 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1250148 | Cytotoxicity against human Glioma cells (HF2381) after 72 hrs by CelltiterGlo assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. |
| AID1623571 | Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in Akt phosphorylation at Ser473 residues at 0.25 to 1 uM after 4 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1421731 | Inhibition of PI3Kgamma (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors. |
| AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1629276 | Antiparasitic activity against bloodstream form of Trypanosoma brucei 221 infected in mouse VSMC assessed as reduction in log10 RLU at 1 uM after 48 hrs by luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19
| Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. |
| AID1568311 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID729011 | Inhibition of mTOR (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1424972 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1427066 | Inhibition of PI3K p110delta (unknown origin) using PIP2 as substrate after 1 hr by ADP-Glo kinase assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
| AID1276305 | Inhibition of ATM (unknown origin) | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents. |
| AID1883106 | Inhibition of PI3Kdelta in rat Rat1 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 1 hr by cellular assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID1300659 | Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 24 hrs by Z2 coulter counter method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Straightforward synthesis of a novel ring-fused pyrazole-lactam and in vitro cytotoxic activity on cancer cell lines. |
| AID1406825 | Inhibition of PI3K-beta (unknown origin) after 40 mins by Kinase-Glo assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship. |
| AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID765568 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and anticancer activity evaluation of a series of [1,2,4]triazolo[1,5-a]pyridinylpyridines in vitro and in vivo. |
| AID1871781 | Inhibition of PI3Kbeta (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review. |
| AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425080 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857279 | Inhibition of N-terminal FLAG-tagged recombinant human mTOR (1362 to end residue) using ULight-4EBP1 peptide as substrate incubated for 30 mins in presence of ATP by Lance ultra assay | | | |
| AID1427064 | Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
| AID1238955 | Inhibition of PI3Kbeta (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424942 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1565366 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1883108 | Binding affinity to tubulin in human A2058 cells assessed as condensed DNA score at 5 uM measured after 6 hrs by DiffQuick staining based microscopic analysis | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID1424986 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1433192 | Inhibition of mTOR (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
| AID1185483 | Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Click chemistry inspired synthesis and bioevaluation of novel triazolyl derivatives of osthol as potent cytotoxic agents. |
| AID1623552 | Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1379445 | Growth inhibition of human T47D cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1303588 | Potentiation of 1.25 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.25 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1396673 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr by Kinase-Glo luminescent assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity. |
| AID1152717 | Effect on phosphatidylcholine level in Trypanosoma brucei brucei Lister 427 at 200 nM after 12 hrs by ES-MS analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1424964 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1883104 | Inhibition of PI3Kalpha in rat Rat1 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 1 hr by cellular assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID1568312 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1421728 | Inhibition of wild type PI3Kalpha (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors. |
| AID1389657 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID648358 | Growth inhibition of human NCI-H483 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1600814 | Antiproliferative activity against human HCT116 cells by MTT assay | | | |
| AID1152718 | Antitrypanosomal activity against bloodstream Trypanosoma brucei brucei Lister 427 after 70 hrs by resazurin assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1424968 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425122 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1152721 | Inhibition of human recombinant mTOR assessed as inhibition of 4EBP1 phosphorylation after 30 mins by TR-FRET analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1152727 | Solubility of compound in phosphate buffer at pH 7.4 after 1 hr | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1568332 | Antitumor activity against human A549 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 20 mg/kg, ig administered for 30 days measured every 3 days during compound dosing relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1185484 | Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Click chemistry inspired synthesis and bioevaluation of novel triazolyl derivatives of osthol as potent cytotoxic agents. |
| AID1226265 | Inhibition of mTOR (unknown origin) using GFP-4E-BP1 as substrate after 1 hr by TR-FRET assay | 2015 | ACS medicinal chemistry letters, Apr-09, Volume: 6, Issue:4
| Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors. |
| AID1754883 | Inhibition of mTOR (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. |
| AID1152731 | Decrease in phosphotidyl inositol phosphate level in Trypanosoma brucei brucei Lister 427 at 200 nM after 12 hrs by ES-MS analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1178741 | Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents. |
| AID1425034 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648362 | Growth inhibition of human LOXIMVI cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1568336 | Toxicity in BALB/c mouse xenografted with human A549 cells assessed as reduction in body weight at 20 mg/kg, ig administered for 30 days | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1623551 | Inhibition of PI3Kdelta (unknown origin) by ADP-gloassay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425073 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1768749 | Antiproliferative activity against human LM3 cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition. |
| AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1329187 | Selectivity ratio of IC50 for PI3Kgamma (unknown origin) expressed in baculovirus co-expressing p85 to IC50 for PI3Kalpha/p85 iSH2 domain (unknown origin) expressed in baculovirus | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648360 | Growth inhibition of human DMS273 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1568305 | Inhibition of recombinant human full length N-terminal DYKDDDDK-tagged PI3Kgamma (1 to 1102 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1857280 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by Kinase Glo luminescence assay | | | |
| AID1871783 | Inhibition of PI3Kgamma (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review. |
| AID1427068 | Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362-end residues) using ULight-4E-BP1 peptide substrate after 1 hr in presence of ATP by Lance Ultra assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
| AID648356 | Growth inhibition of human NCI-H226 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1637617 | Inhibition of PI3Kdelta (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay | 2016 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
| Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors. |
| AID1623567 | Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 71.08%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1425084 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648352 | Growth inhibition of human HT-29 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1623565 | Induction of apoptosis in human Ramos cells assessed as viable cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 96.83%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1245325 | Inhibition of p110gamma/PIK3R5 (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1857281 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate incubated for 2 hrs in presence of ATP by Kinase Glo luminescence assay | | | |
| AID1706187 | Inhibition of PI3Kdelta (unknown origin) by ADP-Glo kinase assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1186550 | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
| Synthesis and biological evaluation of novel isoxazoles and triazoles linked 6-hydroxycoumarin as potent cytotoxic agents. |
| AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425015 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1379443 | Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1425072 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425172 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1178742 | Inhibition of PI3K/Akt signalling in human HCT116 cells assessed as reduction in AKT Ser473 phosphorylation at 1 uM after 1 hr by Western blot method | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents. |
| AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1871782 | Inhibition of PI3Kdelta (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review. |
| AID1389664 | Inhibition of N-terminal His6-tagged recombinant full-length PI3Kbeta (unknown origin)/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 insect cells by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1381743 | Cytotoxicity against human SNU638 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1857334 | Antitumor activity against human SW620 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, IG administered daily for 30 days and measured every 2 days relative to control | | | |
| AID1186552 | Cytotoxicity against human HL60 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
| Synthesis and biological evaluation of novel isoxazoles and triazoles linked 6-hydroxycoumarin as potent cytotoxic agents. |
| AID1754884 | Inhibition of HDAC6 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. |
| AID1424994 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1303587 | Potentiation of 0.25 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.05 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1509605 | Inhibition of PI3K/AKT/mTOR signaling in human HCT116 cells assessed as decrease in AKT phosphorylation at S473 at 1 uM measured after 5 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
| Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1425100 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1379448 | Growth inhibition of human Pfeiffer cells by CCK8 assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1329066 | Inhibition of mTOR (unknown origin) expressed in baculovirus after 60 mins by kinase-glo assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1238958 | Inhibition of mTOR (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1329063 | Inhibition of PI3Kbeta (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 60 mins by kinase-glo assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1637618 | Inhibition of PI3Kgamma (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay | 2016 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
| Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors. |
| AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857283 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate incubated for 2 hrs in presence of ATP by Kinase Glo luminescence assay | | | |
| AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1186553 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
| Synthesis and biological evaluation of novel isoxazoles and triazoles linked 6-hydroxycoumarin as potent cytotoxic agents. |
| AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1637613 | Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
| Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors. |
| AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425198 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID626740 | Antitumor activity in PTEN-deficient human U87MG xenografted in Rag1-/- mouse assessed as inhibition of tumor growth at 15 mg/kg, ip qd for 10 days measured after 10 days (Rvb = 18.5 +/- 3.4%) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474). |
| AID1152730 | Effect on phosphotidyl inositol level in Trypanosoma brucei brucei Lister 427 at 200 nM after 12 hrs by ES-MS analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID748658 | Anticancer activity against mouse BA/F3 cells expressing JAK2 V617F mutation allografted in Harlan SCID mouse assessed as mean survival days at 45 mg/kg, po by luciferase reporter gene assay (Rvb = 16 days) | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Combination Therapy: JAK PI3K/mTOR. A Novel Approach for Cancer Treatment. |
| AID1263095 | Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide as substrate after 1 hr by lance ultra assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857285 | Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | | | |
| AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1568316 | Inhibition of recombinant human full length N-terminal GST-tagged PI3Kalpha (1 to 1068 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 1 hr by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1303594 | Potentiation of 1.25 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.25 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1593870 | Clearance in C57BL/6J mouse at 1 mg/kg, iv measured up to 30 hrs by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1152733 | Antitrypanosomal activity against bloodstream Trypanosoma brucei brucei Lister 427 assessed as decrease in number of cell at G1 phase after 18 hrs by PI staining based flow cytometer | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1263096 | Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID1425074 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1768747 | Antiproliferative activity against human HL7702 cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition. |
| AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1623564 | Induction of apoptosis in human Ramos cells assessed as necrotic cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 1.11%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID648359 | Growth inhibition of human A549 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425090 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1389659 | Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1152729 | Effect on sphingomylein level in Trypanosoma brucei brucei Lister 427 at 200 nM after 12 hrs by ES-MS analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1396653 | Inhibition of recombinant human PI3K-alpha using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors. |
| AID1406828 | Inhibition of mTORC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship. |
| AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1593873 | Oral bioavailability in C57BL/6J mouse at 3 mg/kg measured up to 30 hrs by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1152726 | Lipophilicity, log D of the compound at pH 7.4 by HPLC analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1381740 | Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648340 | Growth inhibition of human BSY1 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1329065 | Inhibition of PI3Kdelta (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 120 mins by kinase-glo assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1565370 | Inhibition of PI3Kbeta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID1303592 | Potentiation of 0.125 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.025 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1329064 | Inhibition of PI3Kgamma (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 120 mins by kinase-glo assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1185486 | Cytotoxicity against human NCI-H322 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Click chemistry inspired synthesis and bioevaluation of novel triazolyl derivatives of osthol as potent cytotoxic agents. |
| AID1593854 | Inhibition of human PI3Kbeta using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1185489 | Cytotoxicity against human A431 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Click chemistry inspired synthesis and bioevaluation of novel triazolyl derivatives of osthol as potent cytotoxic agents. |
| AID1381739 | Cytotoxicity against human BT549 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1303586 | Potentiation of 0.125 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 0.025 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648365 | Growth inhibition of human OVCAR5 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857282 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by Kinase Glo luminescence assay | | | |
| AID1425096 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648339 | Growth inhibition of human HBC4 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425020 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648346 | Growth inhibition of human SF295 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1329186 | Selectivity ratio of IC50 for PI3Kbeta (unknown origin) expressed in baculovirus co-expressing p85 to IC50 for PI3Kalpha/p85 iSH2 domain (unknown origin) expressed in baculovirus | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
| AID1425061 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1381744 | Inhibition of EGFR (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr by mobility shift assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1389660 | Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1238952 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1321993 | Inhibition of PI3Kalpha (unknown origin) using substrate PI incubated for 1 hr by Adapta kinase assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1433191 | Inhibition of P110delta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
| AID1381747 | Inhibition of PI3K p110gamma (unknown origin) using PIP2 as substrate by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1238949 | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1245323 | Inhibition of p110alpha/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 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. |
| AID1509592 | Antiproliferative activity against human MCF7 cells harboring PIK3CA mutant E545K measured after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
| Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1565371 | Inhibition of PI3Kgamma (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID1425109 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1398711 | Antiproliferative activity against human Raji cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425129 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1389655 | Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1425199 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425180 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1593855 | Inhibition of human PI3Kgamma using PIP2 as substrate after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID648361 | Growth inhibition of human DMS114 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1706197 | Inhibition of PI3Kgamma (unknown origin) | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1238951 | Cytotoxicity against human U87MG cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1568304 | Inhibition of recombinant human full length N-terminal GST-tagged PI3Kbeta (1 to 1070 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1178740 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents. |
| AID1424915 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857286 | Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | | | |
| AID1883109 | Binding affinity to tubulin in human A2058 cells assessed as condensed DNA score at 5 uM measured after 24 hrs by DiffQuick staining based microscopic analysis | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425211 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1389666 | Inhibition of recombinant N-terminal full length human PI3K p110delta/recombinant untagged full length human p85alpha expressed in baculovirus infected Sf21 insect cells by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1433189 | Inhibition of P110beta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
| AID648502 | Growth inhibition of human MKN45 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857289 | Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | | | |
| AID1152728 | Apparent permeability across artificial membrane after 3 hrs by HPLC analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1433186 | Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
| AID1396658 | Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors. |
| AID1398704 | Inhibition of PI3Kalpha (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID648353 | Growth inhibition of human HCT15 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID648345 | Growth inhibition of human SF268 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1186549 | Cytotoxicity against human PC3 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
| Synthesis and biological evaluation of novel isoxazoles and triazoles linked 6-hydroxycoumarin as potent cytotoxic agents. |
| AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648355 | Growth inhibition of human NCI-H23 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1238957 | Inhibition of PI3Kdelta (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1186551 | Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
| Synthesis and biological evaluation of novel isoxazoles and triazoles linked 6-hydroxycoumarin as potent cytotoxic agents. |
| AID1593877 | Toxicity in DBA1/J mouse assessed as reduction in body weight at 60 mg/kg, po administered for 14 days measured thrice per week | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1424916 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1398703 | Inhibition of PI3K/Akt/mTOR pathway in human K562 cells assessed as reduction in Akt phosphorylation at Ser-473 residue at 1 uM after 24 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1185485 | Cytotoxicity against human T47D cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Click chemistry inspired synthesis and bioevaluation of novel triazolyl derivatives of osthol as potent cytotoxic agents. |
| AID1427062 | Inhibition of PI3K p110alpha/p85alpha (unknown origin) using PIP2 as substrate after 1 hr by luminescent kinase-Glo assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
| AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1321995 | Inhibition of human recombinant Vps34 using substrate PI incubated for 1 hr by Adapta kinase assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1389663 | Inhibition of recombinant N-terminal His6-tagged full length PI3K p110alpha (unknown origin)/recombinant untagged full length p85alpha (unknown origin) expressed in baculovirus infected Sf21 insect cells by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1424952 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1406823 | Inhibition of recombinant full length PI3K p110alpha/p85alpha (unknown origin) expressed in baculovirus infected sf9 cells using PIP2 as substrate preincubated for 10 mins followed by ATP addition and measured after 45 mins by HTRF assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship. |
| AID1629988 | Inhibition of human mTOR after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counting | 2016 | ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
| Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors. |
| AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857331 | Antitumor activity against human HeLa cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, IG administered daily for 30 days and measured every 2 days relative to control | | | |
| AID1396655 | Inhibition of recombinant human PI3K-gamma using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors. |
| AID1425135 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425189 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID728986 | Inhibition of PI3K (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors. |
| AID1398709 | Inhibition of mTOR (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ. |
| AID1425137 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1662434 | Inhibition of mTOR (unknown origin) | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators. |
| AID701552 | Inhibition of PI3Kalpha | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Recent results in protein kinase inhibition for tropical diseases. |
| AID1185487 | Cytotoxicity against human A549 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Click chemistry inspired synthesis and bioevaluation of novel triazolyl derivatives of osthol as potent cytotoxic agents. |
| AID1238950 | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
| Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea. |
| AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1593868 | Cmax in C57BL/6J mouse at 3 mg/kg, po measured up to 30 hrs by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648369 | Growth inhibition of human ACHN cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1425115 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1706188 | Antiproliferative activity against human Raji cells assessed as inhibition of cell growth after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1424925 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1245334 | Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1381746 | Inhibition of PI3K p110beta (unknown origin) using PIP2 as substrate by ELISA | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1381738 | Cytotoxicity against human A549 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425169 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425158 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1568308 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1593856 | Inhibition of mTOR (unknown origin) assessed as reduction in p70S6K phosphorylation | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1509590 | Inhibition of PI3K delta (unknown origin) using lipid substrate measured after 40 mins in presence of ATP by Kinase-Glo plus reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
| Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1389665 | Inhibition of recombinant human N-terminal His6-tagged full length PI3K p120gamma expressed in baculovirus infected Sf21 insect cells by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3Kα inhibition. |
| AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1509591 | Antiproliferative activity against human HCT116 cells harboring PIK3CA mutant H1047R measured after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
| Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors. |
| AID1568310 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID752996 | Antitumor activity against human U87MG cells xenografted in rag1-deficient mouse assessed as tumor growth inhibition at 15 mg/kg, ip qd measured after 14 days relative to control | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474). |
| AID701550 | Inhibition of mTOR | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Recent results in protein kinase inhibition for tropical diseases. |
| AID1623563 | Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 5 uM after 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 0.98%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1637615 | Inhibition of PI3Kalpha (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assay | 2016 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
| Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors. |
| AID1152719 | Cytotoxicity against human HepG2 cells after 48 hrs by Celltiter-Glo assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness. |
| AID1629986 | Inhibition of recombinant PI3Kbeta (unknown origin) using phosphatidyl inositol as substrate after 30 to 60 mins in presence of ATP by Kinase Glo luminescence assay | 2016 | ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
| Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors. |
| AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID701555 | Inhibition of PI3Kgamma | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Recent results in protein kinase inhibition for tropical diseases. |
| AID1303595 | Potentiation of 2.5 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as combination index at 0.5 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1379439 | Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 hr by ADP-Glo luminescence assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID648347 | Growth inhibition of human SF539 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1883105 | Inhibition of PI3Kbeta in rat Rat1 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 1 hr by cellular assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID1565372 | Inhibition of PI3Kdelta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1381742 | Cytotoxicity against human SKHEP1 cells after 72 hrs by SRB assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα. |
| AID1396654 | Inhibition of recombinant human PI3K-beta using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors. |
| AID1178745 | Toxicity in human HCT116 cells xenografted BALB/C mouse assessed as weight loss at 30 mg/kg, po dosed once daily for 14 days | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents. |
| AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1706189 | Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1425183 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID765570 | Antiproliferative activity against human U87MG cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and anticancer activity evaluation of a series of [1,2,4]triazolo[1,5-a]pyridinylpyridines in vitro and in vivo. |
| AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425009 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425079 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1623568 | Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 5 uM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 4.26%) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1425038 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425207 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425099 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648351 | Growth inhibition of human KM12 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1568330 | Antitumor activity against human HeLa cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 20 mg/kg, ig administered for 30 days measured every 3 days during compound dosing relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1706186 | Inhibition of PI3Kdelta (unknown origin) at 200 nM by ADP-Glo kinase assay relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. |
| AID1427063 | Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
| AID1245335 | Antiproliferative activity against human U87MG cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1245336 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1379447 | Growth inhibition of human KARPAS422 cells by CCK8 assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID1303590 | Potentiation of 7 nM (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as fraction ratio affected at 1.4 uM after 48 hrs by cell titer-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synergistic potentiation of (-)-lomaiviticin A cytotoxicity by the ATR inhibitor VE-821. |
| AID1565365 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα. |
| AID1593872 | AUC (0 to infinity) in C57BL/6J mouse 1 mg/kg, iv measured up to 30 hrs by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors. |
| AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425054 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1857290 | Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | | | |
| AID1568314 | Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362 to end residues) using Ulight-4E-BP1 as substrate incubated for 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID1623572 | Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in mTOR phosphorylation at Ser2481 residues at 0.25 to 1 uM after 4 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ. |
| AID1857288 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | | | |
| AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1245333 | Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
| Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
| Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4
| Navigating the kinome. |
| AID1799847 | TR-FRET Assay from Article 10.1021/bi100673c: \\Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.\\ | 2010 | Biochemistry, Oct-05, Volume: 49, Issue:39
| Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. |
| AID1799846 | Radiometric Filtration Assay from Article 10.1021/bi100673c: \\Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.\\ | 2010 | Biochemistry, Oct-05, Volume: 49, Issue:39
| Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. |
| AID1345726 | Human mechanistic target of rapamycin kinase (FRAP subfamily) | 2008 | Molecular cancer therapeutics, Jul, Volume: 7, Issue:7
| Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. |
| AID1345749 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases) | 2008 | Molecular cancer therapeutics, Jul, Volume: 7, Issue:7
| Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. |
| AID1345786 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases) | 2008 | Molecular cancer therapeutics, Jul, Volume: 7, Issue:7
| Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. |
| AID1345671 | Human ATR serine/threonine kinase (ATR subfamily) | 2011 | Nature structural & molecular biology, Jun, Volume: 18, Issue:6
| A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. |
| AID1345748 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases) | 2008 | Molecular cancer therapeutics, Jul, Volume: 7, Issue:7
| Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |