| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1756630 | Inhibition of Nedd4 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| 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. |
| AID1823489 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| 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. |
| AID1823480 | Antiproliferative activity against human HEK293T cells assessed as reduction in cell viability at 10 uM measured after 72 hrs by Celltiter-Glo luminescent assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1750468 | Inhibition of CK2 (unknown origin) | | | |
| AID566169 | Volume of distribution at steady state in Beagle dog at 1.9 mg/kg, iv and 8.2 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1756587 | Inhibition of Ddx21 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1823479 | Antiproliferative activity against human FaDu cells assessed as reduction in cell viability at 10 uM measured after 72 hrs by Celltiter-Glo luminescent assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| 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. |
| AID1614884 | Binding affinity to CK2alpha (unknown origin) at 100 uM in presence of AMP-PNP by STD-based NMR spectroscopy | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site. |
| AID566160 | AUC in ICR mouse at 25 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1823485 | Induction of apoptosis in human CAL-27 cells assessed as BCL-xL level at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| 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. |
| AID566126 | Inhibition of human recombinant HIPK3 by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| 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. |
| AID1756601 | Inhibition of Ehd2 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| AID1614747 | Inhibition of recombinant human GST-tagged CK2alpha in presence of ATP by radiometric kinase assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID1831597 | Toxicity in nude BALB/c mouse xenografted with human MDA-MB-231 cells assessed as change in body weight at 50 mg/kg, po containing 1:1 compound : JQ-1 ratio administered once daily for 19 days and measured every 3 days | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| 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. |
| AID566140 | Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1750429 | Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.1%) | | | |
| 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. |
| 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. |
| AID1750400 | Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| 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. |
| AID688148 | Cytotoxicity against human LNCAP cells assessed as cell viability at 1 to 10 uM after 1 day by luciferase assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID1705051 | Inhibition of recombinant human CK2alpha' in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID566141 | Antiproliferative activity against human A549 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1846313 | Inhibition of human recombinant CK2alpha | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Recent advances in development of hetero-bivalent kinase inhibitors. |
| 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. |
| 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. |
| AID1750428 | Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1%) | | | |
| 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. |
| 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. |
| AID1070730 | Antimigratory activity against human A549 cells after 24 hrs by wound-healing assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| AID566144 | Antiproliferative activity against human K562 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1652194 | Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
| 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. |
| 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. |
| AID1823486 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 0.5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID566166 | AUC in Sprague-Dawley rat at 10.5 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| 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. |
| AID1750392 | Selectivity index, ratio of IC50 for inhibition of human CLK2 to IC50 for inhibition of human CK2 | | | |
| 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. |
| 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. |
| AID1756625 | Inhibition of LAP2B epsilon in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID1275907 | Inhibition of GST-tagged human CK2alpha' (1 to 350 residues) using CK2tide as substrate incubated for 1 hr by off-chip mobility shift assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
| Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors. |
| AID1481167 | Inhibition of CK2alpha (unknown origin) (1 to 335 residues) using 5-TAMRA-RADDSDDDDD as substrate after 30 mins by fluorescence imaging method | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Oligo-aspartic acid conjugates with benzo[c][2,6]naphthyridine-8-carboxylic acid scaffold as picomolar inhibitors of CK2. |
| 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. |
| 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. |
| AID1823488 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| AID757710 | Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| 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. |
| AID1705050 | Inhibition of recombinant human CK2alpha in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID1294144 | Inhibition of recombinant human CK2 holoenzyme using RRRDDDSDDD as substrate measured after 20 mins at 30 degC by radiometric kinase assay in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design and synthesis of novel protein kinase CK2 inhibitors on the base of 4-aminothieno[2,3-d]pyrimidines. |
| AID1705053 | Inhibition of recombinant human FLT3 in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| 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. |
| AID1851270 | Inhibition of human CLK3-4 (275 to 632 residues) expressed in Escherichia coli BL21 (DE3) Turner using S6-peptide as substrate incubated for 60 mins in presence of [gamma-32P]ATP by radiometric kinase assay | 2022 | Bioorganic & medicinal chemistry, 09-15, Volume: 70 | Exploring the roles of the Cdc2-like kinases in cancers. |
| 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. |
| 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. |
| 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. |
| AID688030 | Cytotoxicity against human LNCAP cells assessed as cell viability after 4 days by CCK8 method | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| 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. |
| AID566121 | Inhibition of human recombinant CK2alpha at enzyme-substrate complex by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1831590 | Antitumor activity against human MDA-MB-468 cells xenografted in po dosed nude BALB/c mouse assessed as tumor growth inhibition at 1:1 JQ-1 : compound ratio administered once daily for 19 days and measured every 3 days | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID688143 | Inhibition of CK2 in human LNCAP cells assessed as androgen receptor activation after 1 day by luciferase assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID688160 | Inhibition of CK2alpha in human LNCAP cells assessed as reduction of XIAP expression at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID688027 | Cytotoxicity against human RWPE1 cells assessed as cell viability at 10 uM after 3 days by CCK8 method | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1425195 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID684572 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds. |
| AID1614841 | Non-ATP competitive binding affinity to GST-tagged CK2alpha (unknown origin) assessed as melting temperature at 6.25 uM by temperature-dependent circular dichroism (Rvb = 53.2 degC) | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site. |
| 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. |
| AID566153 | Inhibition of CYP2D6 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1898572 | Binding affinity to human recombinant CK2alpha2beta2 using RRRDDDSDDD peptide as substrate in presence of [gamma-33P]ATP incubated for 40 mins by radiometric assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Molecular Plasticity of Crystalline CK2α' Leads to KN2, a Bivalent Inhibitor of Protein Kinase CK2 with Extraordinary Selectivity. |
| AID1652189 | Inhibition of human recombinant CK2 using RRRDDDSDDD peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by ADP-Glo kinase assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
| 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. |
| AID1126692 | Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| 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. |
| AID1750430 | Induction of apoptosis in human HCT116 cells assessed as necrotic cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 5.6%) | | | |
| 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. |
| AID1823509 | Inhibition of ATR (unknown origin) in human CAL-27 cells measured after 6 hrs by select screen kinase assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1705057 | Inhibition of recombinant human PIM1 in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID1756604 | Inhibition of Srrm1 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID1756594 | Inhibition of Cep170 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1126693 | Inhibition of CK2alpha1 (unknown origin) using casein as substrate in presence of [gamma33P]ATP | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| 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. |
| AID566130 | Inhibition of human recombinant AKT at 0.5 uM by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID630589 | Inhibition of human recombinant CK2 using RRRDDDSDDD as substrate by radiometric assay in the presence of 15 uM [ATP] | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. |
| AID1070715 | Inhibition of CK2-mediated MMP2 activation in human A549 cells at 30 uM after 48 hrs by gelatin-zymography | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| AID1070732 | Cytotoxicity against human A549 cells assessed as viable cells at 1 to 30 uM after 24 hrs by CCK8 assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| AID566171 | Cmax in Beagle dog at 8.2 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID566167 | Oral bioavailability in Sprague-Dawley rat at 10.5 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1756621 | Inhibition of Plcd3 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1823493 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| AID1756635 | Inhibition of HNRNPC in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID688151 | Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent DHT-induced TMPRSS2 mRNA expression after 8 hrs by real time PCR analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| AID1705056 | Inhibition of recombinant human HIPK3 in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| 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. |
| AID1756632 | Inhibition of NEMF in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID688147 | Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent PSA mRNA level at 10 uM after 8 hrs by real time PCR analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| AID1705054 | Inhibition of recombinant human TBK1 in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID757711 | Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| AID566173 | Oral bioavailability in Beagle dog at 8.2 mg/kg by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1420050 | Inhibition of CK2 (unknown origin) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| 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. |
| AID566147 | Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1614784 | Inhibition of human recombinant DyrK1a by fluorescence-based immunoassay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID1750451 | Tmax in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| 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. |
| AID1750401 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| 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. |
| 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. |
| 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. |
| AID1750453 | Half life in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| AID1756607 | Inhibition of Gbf1 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID688158 | Inhibition of CK2alpha in human LNCAP cells assessed as reduction of p21 phosphorylation at threonine145 at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID566139 | Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1614781 | Inhibition of recombinant human CK2alpha using RRRDDDSDDD substrate and [gamma-33P]ATP by scintillation counting method | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID1409609 | Cytotoxicity of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| 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. |
| AID566161 | Oral bioavailability in ICR mouse at 25 mg/kg by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1823462 | Inhibition of DYRK1A (unknown origin) measured after 6 hrs in presence of ATP by Z'-LYTE assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| AID1823482 | Induction of apoptosis in human CAL-27 cells assessed as PARP level at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| AID1831538 | Inhibition of CK2 (unknown origin) | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1756631 | Inhibition of Usp10 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1424951 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1750459 | MRT(0 to infinity) in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| AID1831526 | Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| 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. |
| AID1070717 | Antimigratory activity against human H1299 cells after 24 hrs by wound-healing assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| AID1876316 | Antiviral activity against SARS-CoV-2 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
| 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. |
| AID1070723 | Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| AID1070726 | Reduction in MMP2 expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1070731 | Cytotoxicity against human A549 cells assessed as viable cells at 1 to 30 uM after 24 hrs by LDH assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| AID1750402 | Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| AID1481164 | Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Oligo-aspartic acid conjugates with benzo[c][2,6]naphthyridine-8-carboxylic acid scaffold as picomolar inhibitors of CK2. |
| AID1614861 | Inhibition of recombinant human CLK2 in presence of ATP by radiometric filter-binding assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site. |
| 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. |
| 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. |
| AID1831535 | Inhibition of BRDT BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1652197 | Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
| AID688163 | Inhibition of CK2alpha in human LNCAP cells assessed as effect on DR5 expression at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID1756639 | Inhibition of CK2 in mouse C2C12 cells assessed as reduction in CDC37 phosphorylation at S13 residues at 1 to 4 uM by Western blot analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1750418 | Inhibition of cell stemness in human HCT116 cells assessed as morphological alterations at 5 uM after 10 days by microscopic analysis | | | |
| 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. |
| AID1070721 | Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| AID1070720 | Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 4 to 24 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| AID757703 | Selectivity index, ratio of CC50 for human PHA-activated PBMC to CC50 for human Jurkat cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| AID757707 | Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| 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. |
| 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. |
| AID1392843 | Inhibition of CK2alpha (unknown origin) (2 to 329 residues) expressed in Escherichia coli BL21 (DE3) using RRRADDSDDDD substrate incubated for 40 mins by ADP-Glo kinase assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| Novel non-ATP competitive small molecules targeting the CK2 α/β interface. |
| AID1614783 | Selectivity index, ratio of IC50 for N-terminal GST-tagged human CLK2 (138 to end residues) to IC50 for recombinant human CK2alpha | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| 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. |
| AID757706 | Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| AID1070719 | Inhibition of CK2-mediated AKT phosphorylation in human A549 cells after 4 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| 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. |
| AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID566162 | Clearance in Sprague-Dawley rat at 5.2 mg/kg, iv and 10.5 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1823492 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1070716 | Antiinvasive activity against human H1299 cells after 3 hrs by Boyden chamber invasion assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1614775 | Inhibition of CK2alpha (unknown origin) assessed as reduction in GST-Six1 phosphorylation in presence of ATP by radiometric kinase assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID688156 | Downregulation of CK2alpha expression in human LNCAP cells assessed as reduction of cytosolic protein level at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID1167185 | Inhibition of human recombinant CK2a1/CK2b holoenzyme expressed in Escherichia coli BL21(DE3) pre-incubated for 10 mins before substrate addition by capillary electrophoresis based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2. |
| AID1409611 | AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID566164 | Elimination half life in Sprague-Dawley rat at 5.2 mg/kg, iv and 10.5 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID566142 | Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1424957 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative 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. |
| AID1614779 | Inhibition EGFP-CK2alpha (unknown origin) expressed in human HeLa cells induction of EGFP-CK2alpha translocation from nucleoli to nuclear matrix and cytoplasm at 8 uM after 12 hrs by Hoechst-33342-staining based microscopy | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| 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. |
| 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. |
| AID1070724 | Inhibition of CK2-mediated MT1-MMP expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| AID1409613 | Selectivity ratio: ratio of AUC (viral infection %) of SARS-CoV-2 in the Vero E6 cell line compared to AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID1756640 | Inhibition of CK2 in mouse C2C12 cells assessed as reduction in CK2 substrates phosphorylation at 1 to 4 uM by Western blot analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1070729 | Antiinvasive activity against human A549 cells after 3 hrs by Boyden chamber invasion assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| AID1614770 | Inhibition of CK2 in human 786-0 cells assessed as decrease in alpha-catenin phosphorylation at Ser641 after 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| 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. |
| 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. |
| AID1756619 | Inhibition of Larp1 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID688150 | Inhibition of CK2 in human LNCAP cells assessed as reduction of DHT-induced androgen receptor dependent TMPRSS2 mRNA expression at 1 to 10 uM after 8 hrs by real time PCR analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1831588 | Antitumor activity against human MDA-MB-231 cells xenografted in po dosed nude BALB/c mouse assessed as tumor growth inhibition at 1:1 JQ-1 : compound ratio administered once daily for 19 days and measured every 3 days | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1831532 | Inhibition of BRD4 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| AID688152 | Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent DHT-induced PSA mRNA expression at 3 uM after 8 hrs by real time PCR analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1652196 | Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
| 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. |
| AID1070713 | Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| AID566120 | Inhibition of human recombinant CK2alpha by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1614863 | Inhibition of recombinant human DYRK1B in presence of ATP by radiometric filter-binding assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site. |
| AID566151 | Inhibition of CYP2C9 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1750455 | AUC(0 to t) in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| AID1420060 | Inhibition of recombinant human DYRK1A by radiometric filter-binding assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID1614785 | Inhibition of human recombinant DyrK1b by fluorescence-based immunoassay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID566174 | Antitumor activity against human PC3 cells xenografted in athymic mouse assessed as tumor growth inhibition at 25 mg/kg, po BID | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1851269 | Inhibition of human CLK2 Long (130 to 496 residues) expressed in Escherichia coli BL21 (DE3) Turner using GSK3 as substrate incubated for 60 mins in presence of [gamma-32P]ATP by radiometric kinase assay | 2022 | Bioorganic & medicinal chemistry, 09-15, Volume: 70 | Exploring the roles of the Cdc2-like kinases in cancers. |
| 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. |
| 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. |
| 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. |
| AID1750452 | Cmax in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| 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. |
| AID1831524 | Inhibition of BRD4 (unknown origin) at 1 uM incubated for 2 hrs by TR-FRET assay relative to control | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1275909 | Thermodynamic solubility of compound in 67 mM phosphate buffer at pH 7.4 after 24 hrs by HPLC analysis | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
| Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors. |
| 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. |
| AID1705052 | Inhibition of recombinant human DAPK3 in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| 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. |
| 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. |
| AID1823490 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 0.5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1756598 | Inhibition of Ktn1 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID1420061 | Inhibition of recombinant human DYRK1B by radiometric filter-binding assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID566131 | Inhibition of human recombinant PDK1 at 0.5 uM by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1846044 | Anticancer activity against mouse Ptch+/- MB55 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| 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. |
| AID1831528 | Inhibition of BRD2 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| AID684571 | Antiproliferative activity against human A549 cells after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds. |
| AID1823487 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| 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. |
| AID566117 | Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID566159 | Cmax in ICR mouse at 25 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1823508 | Inhibition of CK2 (unknown origin) in human CAL-27 cells measured after 6 hrs by select screen kinase assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| AID1652195 | Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
| 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. |
| AID1823461 | Induction of apoptosis in human CAL-27 cells assessed as increase in cleaved-PARP level at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID688154 | Induction of apoptosis in human LNCAP cells at 30 uM after 72 hrs by AnnexinV staining based fluorescent microscopy | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID1831536 | Inhibition of BRDT BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID566123 | Inhibition of human recombinant FLT3 by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1391108 | Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases. |
| AID566137 | Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID757709 | Inhibition of human recombinant CK2 expressed in Escherichia coli BL21(DE3) using RRRDDDSDDD as substrate after 15 mins by capillary electrophoretic analysis | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| 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. |
| AID1823481 | Inhibition of colony formation in human CAL-27 cells at 1 to 10 uM measured after 10 days by crystal violet staining based assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1831534 | Inhibition of BRD4 BD1/BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1846043 | Anticancer activity against mouse Ptch+/- MB21 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| 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. |
| 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. |
| AID688149 | Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent TMPRSS2 mRNA level at 10 uM after 8 hrs by real time PCR analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID566134 | Inhibition of PIM1 at 10 uM by cell-based assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1852786 | Growth inhibition of human HCT116 cells measured after 72 hrs by sulforhodamine B assay | 2022 | RSC medicinal chemistry, Nov-16, Volume: 13, Issue:11
| A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action. |
| AID688029 | Cytotoxicity against human RWPE1 cells assessed as cell viability after 1 to 3 days by CCK8 method | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID1070714 | Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| AID1756637 | Inhibition of Anapc4 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1756593 | Inhibition of Trmt1 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1614782 | Inhibition of N-terminal GST-tagged human CLK2 (138 to end residues) using SR-rich substrate and [gamma-33P]ATP incubated for 40 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID1756592 | Inhibition of Atg9a in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID757702 | Selectivity index, ratio of CC50 for human PHA-activated PBMC to CC50 for human U937 cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| AID1750391 | Inhibition of human CLK2 incubated for 2 hrs | | | |
| 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. |
| AID1756628 | Inhibition of Washc2 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1409607 | IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells). | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| 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. |
| AID688026 | Induction of apoptosis in human LNCAP cells assessed as increase in caspase3 activation at >10 uM after 1 to 2 days | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| AID688144 | Inhibition of CK2 in human LNCAP cells assessed as DHT-induced androgen receptor nuclear translocation preincubated for 9 hrs prior to DHT challenge measured after 3 hrs by Alexa Fluor 488 staining based fluorescence assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID566157 | Volume of distribution at steady state in ICR mouse at 5 mg/kg, iv and 25 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1750408 | Inhibition of ALDH1A1 in human HCT116 cells at 5 uM after 24 hrs by aldefluor staining based fluorescence analysis | | | |
| AID1750399 | Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| 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. |
| AID1756636 | Inhibition of Ncapd2 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID1070722 | Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 15 to 30 mins by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| AID566163 | Volume of distribution at steady state in Sprague-Dawley rat at 5.2 mg/kg, iv and 10.5 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID688145 | Inhibition of CK2 in human LNCAP cells assessed as androgen receptor nuclear translocation at 1 to 10 uM after 12 hrs by Alexa Fluor 488 staining based fluorescence assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| AID688159 | Inhibition of CK2alpha in human LNCAP cells assessed as reduction of Akt phosphorylation at Ser473 at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| AID1756617 | Inhibition of AHNAK in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1756614 | Inhibition of Fermt2 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1409608 | AUC (viral infection %) for SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells). | 2020 | Nature, 07, Volume: 583, Issue:7816
| A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| 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. |
| AID1750441 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 20 uM after 24 hrs by propidium iodide-staining based flow cytometry (Rvb = 14.67%) | | | |
| AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative 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. |
| AID1614777 | Inhibition of CK2 in human 786-0 cells assessed as reduction in STAT3 phosphorylation at Y705 after 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID1756626 | Inhibition of Cdk4 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| AID1070727 | Inhibition of CK2-mediated MMP9 activation in human A549 cells after 48 hrs by gelatin-zymography | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| AID637248 | Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Synthesis and SAR of inhibitors of protein kinase CK2: novel tricyclic quinoline analogs. |
| 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. |
| AID1705058 | Inhibition of recombinant human CDK1/cyclin B in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID1750458 | MRT(0 to t) in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| AID566135 | Inhibition of CDK1 at 10 uM by cell-based assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1756613 | Inhibition of Sec31a in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1750390 | Inhibition of human CK2 incubated for 2 hrs | | | |
| AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1831529 | Inhibition of BRD2 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1737482 | Inhibition of recombinant human CK2alpha (1 to 336 residues) expressed in Escherichia coli BL21 (DE3) using RRADDSDDDD as substrate incubated for 10 mins in presence of [gamma-33P]-ATP by scintillation counting assay | 2020 | European journal of medicinal chemistry, Jun-01, Volume: 195 | A novel class of selective CK2 inhibitors targeting its open hinge conformation. |
| AID1705055 | Inhibition of recombinant human CLK3 in presence of ATP at Km concentration by radiometric filter-binding assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID566136 | Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1704989 | Displacement of fluorescent tracer from full-length human C-terminal NanoLuc-tagged CK2alpha' expressed in HEK293T permeabilized cells measured after 2 hrs by NanoBRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID1750412 | Inhibition of cell stemness in human HCT116 cells assessed as inhibition of CD44+/CD133+ expression at 20 uM after 24 hrs by flow cytometry analysis | | | |
| 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. |
| AID566176 | Antitumor activity against human PC3 cells xenografted in athymic mouse assessed as tumor growth inhibition at 75 mg/kg, po BID | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID566158 | Elimination half life in ICR mouse at 5 mg/kg, iv and 25 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1070728 | Inhibition of CK2-mediated MMP2 activation in human A549 cells after 48 hrs by gelatin-zymography | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| AID566122 | Inhibition of human recombinant DAPK3 by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1425114 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1756608 | Inhibition of Arhgap35 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| 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. |
| AID566132 | Inhibition of human recombinant mTOR at 0.5 uM by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1756618 | Inhibition of Dihydropyrimidinase-related protein 3 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| AID688146 | Inhibition of CK2 in human LNCAP cells assessed as DHT-mediated androgen receptor activation at 1 to 10 uM after 1 day by luciferase assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| AID1750404 | Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| 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. |
| AID1614862 | Inhibition of recombinant human DYRK1A in presence of ATP by radiometric filter-binding assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site. |
| AID630588 | Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 30 uM [ATP] | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. |
| AID688155 | Antiapoptotic activity against human LNCAP cells assessed as cell survival at 10 uM after 1 day by CCK8 method | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID1823491 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1823478 | Antiproliferative activity against human CAL-27 cells assessed as reduction in cell viability at 10 uM measured after 72 hrs by Celltiter-Glo luminescent assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID566170 | Elimination half life in Beagle dog at 1.9 mg/kg, iv and 8.2 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1614774 | Inhibition of CK2beta autophosphorylation (unknown origin) in presence of ATP by radiometric kinase assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| 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. |
| 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. |
| 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. |
| AID566129 | Inhibition of human recombinant PI3K at 0.5 uM by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID566127 | Inhibition of human recombinant PIM1 by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1851271 | Inhibition of human CLK4 (146 to 480 residues) expressed in Escherichia coli BL21 (DE3) Turner using MBP as substrate incubated for 60 mins in presence of [gamma-32P]ATP by radiometric kinase assay | 2022 | Bioorganic & medicinal chemistry, 09-15, Volume: 70 | Exploring the roles of the Cdc2-like kinases in cancers. |
| 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. |
| AID1831527 | Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID566172 | AUC in Beagle dog at 8.2 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1851268 | Inhibition of human CLK1 Long (148 to 484 residues) expressed in Escherichia coli BL21 (DE3) Turner incubated for 60 mins in presence of [gamma-32P]ATP by radiometric kinase assay | 2022 | Bioorganic & medicinal chemistry, 09-15, Volume: 70 | Exploring the roles of the Cdc2-like kinases in cancers. |
| AID1614769 | Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| 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. |
| AID566152 | Inhibition of CYP2C19 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID566168 | Clearance in Beagle dog at 1.9 mg/kg, iv and 8.2 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| 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. |
| AID1823458 | Induction of apoptosis in human CAL-27 cells assessed as increase in cleaved-PARP level at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| AID566150 | Inhibition of CYP1A2 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID566138 | Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1704986 | Displacement of fluorescent tracer from full-length human C-terminal NanoLuc-tagged CK2alpha expressed in HEK293T cells measured after 2 hrs by NanoBRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID757708 | Cytotoxicity against human PHA-activated PBMC after 1 to 3 days by MTS assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| 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. |
| AID1750440 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 20 uM after 24 hrs by propidium iodide-staining based flow cytometry (Rvb = 36.43%) | | | |
| AID1750460 | Antitumor activity against human HCT116 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 60 mg/kg, po administered twice daily for 4 weeks and measured every 3 days | | | |
| AID1614776 | Inhibition of CK2alpha (unknown origin) assessed as reduction in nucleolin phosphorylation in presence of ATP by radiometric kinase assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. |
| AID757705 | Selectivity index, ratio of CC50 for human PHA-activated PBMC to CC50 for human K562 cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1756599 | Inhibition of Mcm2 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1750457 | Volume of distribution in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| 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. |
| AID1831598 | Toxicity in nude BALB/c mouse xenografted with human MDA-MB-468 cells assessed as change in body weight at 50 mg/kg, po containing 1:1 compound : JQ-1 ratio administered once daily for 19 days and measured every 3 days | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1275908 | Cytotoxicity against human A549 cells after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
| Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors. |
| AID566125 | Inhibition of human recombinant CLK3 by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID688028 | Cytotoxicity against human LNCAP cells assessed as cell viability at 10 uM by CCK8 method | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1750454 | Clearance in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| 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. |
| 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. |
| AID1831525 | Inhibition of CK2 (unknown origin) at 1 uM relative to control | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| AID1362778 | Displacement of 5-TAMRA-labeled ARC-1530 from CK2alpha (unknown origin) (1 to 335 residues) after 15 to 60 mins by luminescence assay | 2018 | Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
| Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2. |
| 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. |
| AID1275906 | Inhibition of GST-tagged human CK2alpha (1 to 391 residues) using CK2tide as substrate incubated for 1 hr by off-chip mobility shift assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
| Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors. |
| AID630587 | Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 5 uM [ATP] | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. |
| AID1539762 | Inhibition of CK2alpha (unknown origin) using RRRADDSDDDDD as substrate in presence of [gamma33P]-ATP by autoradiography | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Small molecule modulators targeting protein kinase CK1 and CK2. |
| 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. |
| AID684573 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds. |
| AID566128 | Inhibition of human recombinant CDK1/Cyclin B by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| AID1750456 | AUC(0 to infinity) in Sprague-Dawley rat at 25 mg/kg, po measured up to 48 hrs by LC-MS/MS analysis | | | |
| AID1831537 | Inhibition of CK1 (unknown origin) | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| 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. |
| AID566155 | Inhibition of human ERG at 0.1 to 10 uM by patch clamp technique | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1425088 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1846314 | Inhibition of human recombinant CK2alpha' | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Recent advances in development of hetero-bivalent kinase inhibitors. |
| AID1898574 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-based cytotoxicity assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Molecular Plasticity of Crystalline CK2α' Leads to KN2, a Bivalent Inhibitor of Protein Kinase CK2 with Extraordinary Selectivity. |
| 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. |
| AID1167184 | Inhibition of human recombinant CK2a1/CK2b holoenzyme expressed in Escherichia coli BL21(DE3) at 10 uM pre-incubated for 10 mins before substrate addition by capillary electrophoresis based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2. |
| AID757712 | Inhibition of human recombinant CK2 expressed in Escherichia coli BL21(DE3) using RRRDDDSDDD as substrate at 10 uM after 15 mins by capillary electrophoretic analysis relative to control | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| 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. |
| 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. |
| AID566154 | Inhibition of CYP3A4 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID1831530 | Inhibition of BRD3 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| AID566133 | Inhibition of FLT3 at 10 uM by cell-based assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID688157 | Downregulation of CK2alpha expression in human LNCAP cells assessed as reduction of nuclear protein level at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID566145 | Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1070733 | Cytotoxicity against human A549 cells assessed as viable cells at 1 to 30 uM after 3 hrs by CCK8 assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| 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. |
| AID566148 | Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1704987 | Displacement of fluorescent tracer from full-length human C-terminal NanoLuc-tagged CK2alpha' expressed in HEK293T cells measured after 2 hrs by NanoBRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| 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. |
| AID688031 | Inhibition of CK2alpha in human LNCAP cells assessed as reduction of survivin expression at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| 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. |
| AID1823483 | Induction of apoptosis in human CAL-27 cells assessed as PARP level at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| AID1392844 | Inhibition of CLK2 (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| Novel non-ATP competitive small molecules targeting the CK2 α/β interface. |
| AID1070718 | Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 0.15 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| AID1756620 | Inhibition of Phldb1 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1756638 | Inhibition of CK2 in mouse C2C12 cells assessed as reduction in Akt phosphorylation at S129 residues at 1 to 4 uM by Western blot analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1898576 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability at up to 100 uM incubated for 24 hrs by resazurin-based cytotoxicity assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Molecular Plasticity of Crystalline CK2α' Leads to KN2, a Bivalent Inhibitor of Protein Kinase CK2 with Extraordinary Selectivity. |
| 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. |
| AID688162 | Inhibition of CK2alpha in human LNCAP cells assessed as induction of CHOP expression at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID757704 | Selectivity index, ratio of CC50 for human PHA-activated PBMC to CC50 for human MV4-11 cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. |
| AID1750439 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 20 uM after 24 hrs by propidium iodide-staining based flow cytometry (Rvb = 48.89%) | | | |
| 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. |
| AID566165 | Cmax in Sprague-Dawley rat at 10.5 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| 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. |
| 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. |
| AID566149 | Antiproliferative activity against human A375 cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1831533 | Inhibition of BRD4 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| AID1704988 | Displacement of fluorescent tracer from full-length human C-terminal NanoLuc-tagged CK2alpha expressed in HEK293T permeabilized cells measured after 2 hrs by NanoBRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. |
| AID566146 | Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID566143 | Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| 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. |
| AID566124 | Inhibition of human recombinant TBK1 by radiometric assay | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID707263 | Neuroprotective activity against glutamate-induced toxicity in mouse HT22 cells after 24 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1750427 | Induction of apoptosis in human HCT116 cells assessed as viable cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 88.3%) | | | |
| 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. |
| AID1750403 | Cytotoxicity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| AID566177 | Toxicity in athymic mouse xenografted with human PC3 assessed as change in body weight at 25 to 75 mg/kg, po BID | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1756611 | Inhibition of ATRX in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| AID1831531 | Inhibition of BRD3 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
| Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. |
| 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. |
| 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. |
| AID566175 | Antitumor activity against human PC3 cells xenografted in athymic mouse assessed as tumor growth inhibition at 50 mg/kg, po BID | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID566156 | Clearance in ICR mouse at 5 mg/kg, iv and 25 mg/kg, po by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1823484 | Induction of apoptosis in human CAL-27 cells assessed as BCL-xL level at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4
| Selective Macrocyclic Inhibitors of DYRK1A/B. |
| 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. |
| 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. |
| 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. |
| AID688164 | Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor nuclear translocation at 10 uM after 12 to 24 hrs by HCS analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| AID1756634 | Inhibition of SF3b2 in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| AID1846045 | Anticancer activity against mouse Ptch+/- Trp53-/- MB53 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| 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. |
| AID688153 | Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor nuclear translocation at 10 uM after 12 to 24 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells. |
| 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. |
| AID1756633 | Inhibition of ELOA in mouse C2C12 cells assessed as reduction in phospho-sites occupancy at 4 uM after 5 hrs by SILAC based LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Comparing the efficacy and selectivity of Ck2 inhibitors. A phosphoproteomics approach. |
| 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. |
| 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. |
| 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. |
| AID1070725 | Reduction in MMP9 expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells. |
| 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. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| 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. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| 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. |
| AID1345669 | Human death associated protein kinase 3 (Death-associated kinase (DAPK) family) | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1345321 | Human casein kinase 2, alpha 1 polypeptide subunit (Casein kinase 2 (CK2) family) | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1345385 | Human casein kinase 2, alpha prime polypeptide subunit (Casein kinase 2 (CK2) family) | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1345639 | Human homeodomain interacting protein kinase 3 (HIPK subfamily) | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. |
| AID1345734 | Human Pim-1 proto-oncogene, serine/threonine kinase (PIM family) | 2011 | Biochemistry, Oct-04, Volume: 50, Issue:39
| Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |