| Assay ID | Title | Year | Journal | Article |
|---|
| AID1801133 | KinEASE-STK Assay from Article 10.1021/cb500908d: \\Identification and further development of potent TBK1 inhibitors.\\ | 2015 | ACS chemical biology, Jan-16, Volume: 10, Issue:1
| Identification and further development of potent TBK1 inhibitors. |
| AID1799771 | Enzyme Assay from Article 10.1074/jbc.M110.206193: \\Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.\\ | 2011 | The Journal of biological chemistry, May-27, Volume: 286, Issue:21
| Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. |
| AID1801713 | Competition Binding Assays from Article 10.1021/acschembio.5b01063: \\Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5
| Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors. |
| AID1799178 | EGFR IC50 Determination from Article 10.1016/j.bmc.2008.02.053: \\Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.\\ | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
| AID1795774 | Kinase Inhibition Assay from Article 10.1016/j.bmcl.2003.10.010: \\Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.\\ | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
| Synthesis and SAR of potent EGFR/erbB2 dual inhibitors. |
| AID1799179 | Src IC50 Determination from Article 10.1016/j.bmc.2008.02.053: \\Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.\\ | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| AID1715111 | Inhibition of PDGFRA (unknown origin) at 1 uM relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1281898 | Selectivity index, ratio of IC50 for human LO2 cells to human HepG2 cells | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Phosphoramidate protides of five flavones and their antiproliferative activity against HepG2 and L-O2 cell lines. |
| AID481815 | Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. |
| AID436032 | Binding constant for MYO3B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1411551 | Effect on EGFR signaling in human A549 cells assessed as decrease in STAT3 levels at 2 uM after 24 hrs by Cy3 dye-based scanning confocal microscopic analysis | 2017 | MedChemComm, Sep-01, Volume: 8, Issue:9
| Synthesis and biological evaluation of chalcone-linked pyrazolo[1,5- |
| AID1289546 | Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
| AID383035 | Cytotoxicity against human PC14 cells expressing EGFR E746_A750 mutant at 2 uM assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1224749 | Delta TM value showing the stabilisation of CAMK1D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID384142 | Cytotoxicity against human SW13 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383606 | Cytotoxicity against human C-4 II cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384189 | Cytotoxicity against human NCI-H23 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1667576 | Inhibition of HER2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 40 mins in presence of ATP by caliper mobility shift assay | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
| Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold. |
| AID435170 | Binding constant for MYO3A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1730909 | Antiviral activity against DENV-2 New Guinea C infected in human Huh-7 cells measured after 72 hrs by Renilla luciferase reporter gene assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Discovery of 3-phenyl- and 3-N-piperidinyl-isothiazolo[4,3-b]pyridines as highly potent inhibitors of cyclin G-associated kinase. |
| AID1875914 | Inhibition of GAK (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1222793 | Dissociation constant, pKa of the compound | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
| Which metabolites circulate? |
| AID636198 | Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
| Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones. |
| AID1713458 | Metabolic stability in pooled human liver microsomes assessed as Clearance at 3 uM measured up to 45 mins in presence of NADPH by LC-MS/MS analysis | | | |
| AID384371 | Cytotoxicity against human NUGC4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1551767 | Antiproliferation activity against human MCF7 cells assessed as inhibition of cell proliferation at 1 uM by MTT assay relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Design, synthesis and docking studies of benzimidazole derivatives as potential EGFR inhibitors. |
| AID384140 | Cytotoxicity against human SW1116 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256580 | Average Binding Constant for CAMKK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID383892 | Cytotoxicity against human H69V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID383048 | Cytotoxicity against human SNU449 cells expressing wild type EGFR at 2 uM assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383290 | Inhibition of ULK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1250370 | Fraction unbound in Han Wistar rat blood at 5 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID383890 | Cytotoxicity against human H3255 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1566569 | Cytotoxicity against human MCF7 cells by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Developments in the anticancer activity of structurally modified curcumin: An up-to-date review. |
| AID256593 | Average Binding Constant for NEK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1673305 | Binding affinity to T7-tagged EGFR (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK). |
| AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435658 | Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID383644 | Cytotoxicity against human COLO 680N cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1741736 | Cytotoxicity against human PANC-1 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes. |
| AID435780 | Binding constant for BMPR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435200 | Binding constant for full-length TNNI3K | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID384905 | Cytotoxicity against human WiDr cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224760 | Delta TM value showing the stabilisation of CHEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID441997 | Antitumor activity against human A431 cells xenografted in nude mouse assessed as reduction in tumor size at 10 mg/kg, po QD for 11 days | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
| Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung 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. |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID461254 | Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. |
| AID1301726 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| 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. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1317912 | Inhibition of recombinant full length human PRKCA expressed in baculovirus at 500 nM by Z'-LYTE assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Chiral 6-aryl-furo[2,3-d]pyrimidin-4-amines as EGFR inhibitors. |
| AID1224779 | Delta TM value showing the stabilisation of NEK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1713497 | Inhibition of recombinant full length GST-tagged human PIM2 expressed in baculovirus expression system at 500 nM using Ser/Thr 07 as substrate incubated for 1 hr in presence of ATP at its Km concentration by Z'-LYTE assay relative to control | | | |
| AID383597 | Cytotoxicity against human BT483 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID256652 | Average Binding Constant for CAMK2B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID313401 | Growth inhibition of human A431 cells overexpressing EGFR after 72 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
| Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening. |
| 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. |
| AID256674 | Average Binding Constant for PKMYT1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID383598 | Cytotoxicity against human BT549 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1609520 | Induction of apoptosis in human MCF7 cells assessed as increase in apoptosis/necrosis cells at IC50 incubated for 24 hrs by Annexin V-FITC/ethidium homodimer 3 staining based fluorescence microscopic method relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors. |
| AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1544718 | Antiproliferative activity against human A431 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
| Structure based designing of triazolopyrimidone-based reversible inhibitors for kinases involved in NSCLC. |
| AID1612889 | Induction of apoptosis in human A549 cells assessed as increase in TP53 expression at 10 uM after 24 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis, in silico pharmacokinetics prediction and biological evaluation of 1,4-dihydroindeno[1,2-c]pyrazole chalcone as EGFR /Akt pathway inhibitors. |
| AID384673 | Cytotoxicity against human HLE cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1713504 | Inhibition of recombinant human GST-tagged RET (658 to 1114 residues) expressed in baculovirus expression system at 500 nM using Tyr 02 as substrate incubated for 1 hr in presence of ATP at its Km concentration by Z'-LYTE assay relative to control | | | |
| AID1730899 | Antiviral activity against DENV-2 New Guinea C infected in human Huh-7 cells preincubated for 1 hr followed by viral infection and measured after 48 hrs by Renilla luciferase reporter gene assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Discovery of 3-phenyl- and 3-N-piperidinyl-isothiazolo[4,3-b]pyridines as highly potent inhibitors of cyclin G-associated kinase. |
| AID435932 | Binding constant for PKAC-alpha kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1533637 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Antitumoral activity of quinoxaline derivatives: A systematic review. |
| 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. |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1713469 | Inhibition of recombinant human GST-tagged EPHA2 cytoplasmic domain expressed in baculovirus expression system at 500 nM using Tyr 01 peptide as substrate incubated for 1 hr in presence of ATP at its Km concentration by Z'-LYTE assay relative to control | | | |
| AID1261456 | Inhibition of EGFR phosphorylation in human NCI-H292 cells preincubated for 1 hr followed by stimulation with EGF for 8 mins by electrochemiluminescent immunoassay | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study. |
| AID580189 | Inhibition of HER2 by homogeneous time-resolved fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. |
| AID385052 | Cytotoxicity against human DU145 cells at 200 nM assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1578238 | Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | 6-Cinnamoyl-4-arylaminothienopyrimidines as highly potent cytotoxic agents: Design, synthesis and structure-activity relationship studies. |
| AID1609523 | Inhibition of recombinant human N-terminal GST-tagged HER2 (676 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide as substrate incubated for 1 hr by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors. |
| AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID385041 | Cytotoxicity against human PC9 cells at 200 nM assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1917350 | Cytotoxicity against human A-431 cells assessed as inhibition of cell growth at 100 uM incubated for 72 hrs by MTT assay | | | |
| AID435694 | Binding constant for TNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1273724 | Toxicity in zebrafish embryo assessed as kinked tails at 50 and 100 uM | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Extended structure-activity study of thienopyrimidine-based EGFR inhibitors with evaluation of drug-like properties. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1283993 | Inhibition of EGFR-T790M/L858 mutant (unknown origin) preincubated for 30 mins followed by addition of 2x ATP-substrate mixture measured after 1 hr by Kinase Glo luminescent kinase assay | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
| Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors. |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1713453 | Antiproliferative activity against human BXPC-3 cells measured for 96 hrs by sytox green dye staining based proliferation assay | | | |
| AID1224775 | Delta TM value showing the stabilisation of ERK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID384373 | Cytotoxicity against human OAW42 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
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| AID1364452 | Inhibition of EGF-stimulated wild-type EGFR phosphorylation in human A549 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants |
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| AID461268 | Antiproliferative activity against human SCC25 cells | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. |
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| Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones. |
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| DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
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| Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones. |
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| Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones. |
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| Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones. |
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| Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
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| Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| 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
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| 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. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
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| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 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. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |