| Assay ID | Title | Year | Journal | Article |
|---|
| AID364976 | Inhibition of GST tagged human recombinant PI3K C2beta by radiometric scintillation proximity assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID646535 | Selectivity ratio of EC50 for PTEN-null human PC3 cells to EC50 for human MCF7.1 cells expressing PI3Kalpha mutant | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
| Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform. |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1321972 | Inhibition of PI3KC2alpha (unknown origin) | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
| AID1727924 | Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
| 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. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1727899 | Antiproliferative activity against human Calu3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
| AID1861332 | Inhibition of HDAC in human DOHH-2 cells assessed as Down-regulation of STAT3 phosphorylation at Y705 residue at 10 uM measured by Western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
| AID1202611 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1484029 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in presence of ATP by HTRF method | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhib |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1186393 | Inhibition of PDGFRbeta (unknown origin) using poly (Glu, Tyr) 4:1 substrate incubated for 30 mins by HTRF assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents. |
| 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. |
| AID723260 | Inhibition of PI3Kalpha in human SKOV3 cells assessed as inhibition of Akt Ser473 phosphorylation at 1 to 1000 nM after 1 hr by immunoblot analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID648339 | Growth inhibition of human HBC4 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425092 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1484028 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in presence of ATP by HTRF method | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhib |
| AID1361717 | Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| 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. |
| AID602614 | Drug uptake in tumor of nude mouse xenografted with HER2 expressing MCF7 at 50 mg/kg, po administered as single dose after 1 hr | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
| Structure-based design of thienobenzoxepin inhibitors of PI3-kinase. |
| AID364980 | Ratio of IC50 for human recombinant p110beta/p85-alpha PI3K to IC50 for human recombinant p110alpha/p85-alpha PI3K | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1727919 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
| 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. |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1578115 | Inhibition of PI3Kbeta (unknown origin) | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1177098 | Inhibition of human class 3 PI3K by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1
| Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID364972 | Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1702050 | Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID474178 | Antiproliferative activity against human MCF7.1 cells after 3 days by celltiter-glo luminescence assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. |
| AID1361703 | Inhibition of PI4K3A (unknown origin) using PI:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| 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. |
| AID1451363 | Binding affinity to human VPS34 (S282 to H879 residues) expressed in mammalian expression system by Kinomescan assay | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702099 | Inhibition of human PI4kbeta incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID1425005 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702089 | Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| 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. |
| AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID719923 | Selectivity ratio of IC50 for PI3Kgamma to IC50 for PI3Kdelta | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
| PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1702057 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| 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. |
| AID648369 | Growth inhibition of human ACHN cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1172499 | Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents. |
| 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. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1883109 | Binding affinity to tubulin in human A2058 cells assessed as condensed DNA score at 5 uM measured after 24 hrs by DiffQuick staining based microscopic analysis | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1202612 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo. |
| 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. |
| AID364538 | Bioavailability in Beagle dog at 1 mg/kg, iv or 2 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| 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. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID723257 | Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1361702 | Inhibition of N-terminal GST-tagged recombinant human PIK3C2B catalytic domain expressed in Baculovirus expression system using PI as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in presence of 50 uM ATP by ADP-Gl | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
| AID650404 | Inhibition of CYP3A4 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. |
| AID1507124 | Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110delta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Designing multi-targeted agents: An emerging anticancer drug discovery paradigm. |
| AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID650403 | Inhibition of CYP2D6 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1434153 | Cytotoxicity against human MDA-MB-231 cells by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design and synthesis of novel 7-aminosubstituted pyrido[2,3-b]pyrazines exhibiting anti-breast cancer activity. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1659989 | Inhibition of human PI3K p110beta by HTRF assay | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12
| Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives. |
| AID648351 | Growth inhibition of human KM12 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID683640 | Cytotoxicity against human NCI-H1975 cells assessed as growth inhibition after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Design, synthesis and 3D-QSAR analysis of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives as potential antitumor agents. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1727905 | Antiproliferative activity against human NCI-H522 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
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| AID1727920 | Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID364988 | Inhibition of Akt Ser 473 phosphorylation in PTEN-null human PC3 cells | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID1727901 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
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| The target landscape of clinical kinase drugs. |
| AID1202629 | Inhibition of p110alpha/p85alpha (unknown origin) using L-alpha-phosphatidylinositol incubated for 40 mins by ADP depletion detection based luciferase assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1321979 | Inhibition of mTOR (unknown origin) | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
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| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
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| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID723258 | Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhib |
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| The target landscape of clinical kinase drugs. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1186386 | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents. |
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| The target landscape of clinical kinase drugs. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1361719 | Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. |
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| The target landscape of clinical kinase drugs. |
| AID364540 | Volume of distribution at steady state in Beagle dog at 1 mg/kg, iv or 2 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| 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. |
| 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. |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID1482747 | Antiproliferative activity against human SKOV3 cells harboring PIK3CA mutant after 72 hrs by CCK-8 assay | 2017 | Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
| Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID1702072 | Inhibition of human PI3Kbeta incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| The target landscape of clinical kinase drugs. |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID648500 | Growth inhibition of human MKN7 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID648342 | Growth inhibition of human MCF7 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
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| Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. |
| AID632636 | Plasma protein binding in human | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. |
| AID364982 | Inhibition of human Flt3 at 1 uM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1547676 | Synergistic growth inhibition of ALK-negative human A549 cells assessed as combination index at compound:ceritinib concentration ratio of 1:1 and fractional effect of 0.5 in presence of ceritinib by Chou-Talalay method | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID746343 | In vivo inhibition of PI3K in human MCF7-neo/Her2 cells xenografted in taconic nude mouse assessed as decrease in pPRAS40 level in tumor at 100 mg/kg measured at 4 hrs relative to control | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
| Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform. |
| AID464705 | Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID746370 | Inhibition of GST-fused human recombinant PI3Kalpha expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
| Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
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| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID364530 | Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| AID364532 | Metabolic stability in CD1 mouse liver microsomes at 10 uM after 30 mins | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives. |
| AID683638 | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Design, synthesis and 3D-QSAR analysis of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives as potential antitumor agents. |
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| The target landscape of clinical kinase drugs. |
| AID364536 | Oral bioavailability in monkey | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| AID1702090 | Antiproliferative activity against human SNU-398 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1409392 | Inhibition of TORC1 in human SKOV3 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1547678 | Synergistic growth inhibition of ALK-negative human A549 cells assessed as combination index at compound:ceritinib concentration ratio of 1:1 and fractional effect of 0.96 in presence of ceritinib by Chou-Talalay method | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID496760 | Inhibition of p110beta | 2010 | Nature chemical biology, Feb, Volume: 6, Issue:2
| The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. |
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| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702086 | Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| 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. |
| 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. |
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| Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID648505 | Growth inhibition of human PC3 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| 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. |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| 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. |
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| AID1861317 | Inhibition of PI3Kalpha in human DOHH-2 cells assessed as decrease in AKT phosphorylation at 10 uM measured by western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1727904 | Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID699806 | Selectivity ratio of IC50 for PI3Kbeta to IC50 for PI3Kdelta | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1543692 | Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. |
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| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| AID699804 | Selectivity ratio of IC50 for PI3Kgamma to IC50 for PI3Kdelta | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors. |
| AID1915590 | Inhibition of PI3Kalpha (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. |
| AID683641 | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Design, synthesis and 3D-QSAR analysis of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives as potential antitumor agents. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID1202630 | Inhibition of p110beta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol incubated for 40 mins by ADP depletion detection based luciferase assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo. |
| AID1727895 | Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
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| The target landscape of clinical kinase drugs. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID648366 | Growth inhibition of human OVCAR8 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID648340 | Growth inhibition of human BSY1 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| 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. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID650400 | Inhibition of CYP1A2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID648498 | Growth inhibition of human St-4 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID364535 | Oral bioavailability in rat at 10 mg/kg | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1520511 | Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702055 | Inhibition of HDAC1 in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate measured after 2 hrs by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID1306914 | Inhibition of PI3Kalpha (unknown origin) using PI substrate incubated for 60 mins by kinase-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety. |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID648344 | Growth inhibition of human U251 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID364977 | Inhibition of GST tagged human recombinant PI3K Vps34 by radiometric scintillation proximity assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID364981 | Ratio of IC50 for human recombinant p110gamma/p85-alpha PI3K to IC50 for human recombinant p110alpha/p85-alpha PI3K | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1451364 | Binding affinity to human PI4KCbeta (M1 to M828 residues) expressed in mammalian expression system by Kinomescan assay | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. |
| AID648368 | Growth inhibition of human RXF631L cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1883108 | Binding affinity to tubulin in human A2058 cells assessed as condensed DNA score at 5 uM measured after 6 hrs by DiffQuick staining based microscopic analysis | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. |
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| The target landscape of clinical kinase drugs. |
| AID1520572 | Antitumor activity against human RPMI8226 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 75 mg/kg, po administered once per day for 21 days | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID364993 | Decrease in Akt phosphorylation level in human U87MG cells xenografted Ncr athymic mouse at 75 mg/kg, po qd after 1 hr by electrochemiluminescence immunoassay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID732400 | Antitumor activity against KRas mutant, LKB1 deficient human A549 cells xenografted in mouse assessed as tumor growth inhibition at 5 to 30 mg/kg, po qd | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702054 | Inhibition of human PI3Kdelta incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1727918 | Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
| AID1547692 | Cytotoxicity against ALK-negative human A549 cells assessed as cell growth inhibition by Chou-Talalay method | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID732399 | Toxicity in po dosed mouse xenografted with KRas mutant, LKB1 deficient human A549 cells assessed as body weight changes administered qd in presence of MEK inhibitor, GDC-0973 | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. |
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| The target landscape of clinical kinase drugs. |
| AID1578116 | Inhibition of PI3Kdelta (unknown origin) | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. |
| AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID708626 | Ratio of fraction unbound in brain to fraction unbound in plasma in CD-1mouse | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. |
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| The target landscape of clinical kinase drugs. |
| AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID1623289 | Antitumor activity against human U87MG cells xenografted in nude-Fox1nu mouse assessed as tumor growth inhibition at 150 mg/kg bid relative to control | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Recent advances in the discovery of small molecules targeting glioblastoma. |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID632628 | Lipophilicity, log D of the compound | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1186383 | Cytotoxicity against human H460 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents. |
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| The target landscape of clinical kinase drugs. |
| AID1543674 | Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1702077 | Inhibition of human mTOR | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID364984 | Inhibition of human TrkA | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID648353 | Growth inhibition of human HCT15 cells | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
| AID1434154 | Cytotoxicity against human HCC1954 cells by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design and synthesis of novel 7-aminosubstituted pyrido[2,3-b]pyrazines exhibiting anti-breast cancer activity. |
| AID1186395 | Inhibition of KIT (unknown origin) using poly (Glu, Tyr) 4:1 substrate incubated for 30 mins by HTRF assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents. |
| AID1727921 | Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID364995 | Decrease in Akt phosphorylation level in human U87MG cells xenografted Ncr athymic mouse at 75 mg/kg, po qd after 30 mins by electrochemiluminescence immunoassay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| 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. |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1520570 | Antitumor activity against human MM1S cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 75 mg/kg, po administered once per day for 21 days | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
| Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1861333 | Inhibition of HDAC in human OCILY3 cells assessed as Down-regulation of STAT3 phosphorylation at Y705 residue at 10 uM measured by Western blot analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID750504 | AUCtotal in nude mouse at 100 mg/kg, po | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID732401 | Antitumor activity against KRas mutant, LKB1 deficient human A549 cells xenografted in po dosed mouse assessed as delay in tumor growth administered qd in presence of MEK inhibitor, GDC-0973 | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. |
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| The target landscape of clinical kinase drugs. |
| AID364987 | Inhibition of Akt Ser 473 phosphorylation in PTEN-null human U87MG cells | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID364989 | Inhibition of Akt Ser 473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID364990 | Blockade of human ERG channel by whole cell patch clamp assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| 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. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702078 | Inhibition of human PI3K2alpha incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID1451365 | Binding affinity to DNAPK (unknown origin) by Kinomescan assay | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. |
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| The target landscape of clinical kinase drugs. |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID364994 | Decrease in Akt phosphorylation level in human U87MG cells xenografted Ncr athymic mouse at 75 mg/kg, po qd after 4 hrs by electrochemiluminescence immunoassay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID632639 | Antiproliferative activity against human MCF7.1 cells expressing HER2 gene after overnight incubation by CellTiter-Glo luminescence assay | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. |
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| The target landscape of clinical kinase drugs. |
| AID1861309 | Induction of apoptosis in human DOHH-2 cells measured by flow cytometry analysis | 2022 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 71 | Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. |
| AID1379439 | Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 hr by ADP-Glo luminescence assay | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
| Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702141 | Inhibition of HDAC6 in human MCF7 cells assessed as increase in acetylated alpha-tubulin at Lys40 residue incubated for 3 hrs by ELISA | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| AID1547672 | Synergistic growth inhibition of ALK-negative human A549 cells assessed as combination index at compound:ceritinib concentration ratio of 1:1 and fractional effect of 0.25 in presence of ceritinib by Chou-Talalay method | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer. |
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| The target landscape of clinical kinase drugs. |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1202631 | Inhibition of p110gamma/PIK3R5 (unknown origin) using L-alpha-phosphatidylinositol incubated for 40 mins by ADP depletion detection based luciferase assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo. |
| AID1727923 | Antiproliferative activity against human HCC1954 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of |
| 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. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1409391 | Inhibition of TORC2 in human SKOV3 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID750515 | Inhibition of PI3Kalpha (unknown origin) assessed as 3,4,5-inositoltriphosphate formation after 30 mins by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
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| The target landscape of clinical kinase drugs. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1482746 | Antiproliferative activity against PTEN deficient human U87MG cells after 72 hrs by CCK-8 assay | 2017 | Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
| Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1202632 | Inhibition of p110delta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol incubated for 40 mins by ADP depletion detection based luciferase assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo. |
| 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. |
| AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID750500 | Antitumor activity against human MCF7-neo/Her2 cells xenografted in nude mouse at 45 mg/kg, po qd for 20 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust i |
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| JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
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| The target landscape of clinical kinase drugs. |
| AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1617137 | Inhibition of PI3Kgamma (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of |
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| The target landscape of clinical kinase drugs. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
| AID1623288 | Antiproliferative activity against human U87MG cells after 96 hrs | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Recent advances in the discovery of small molecules targeting glioblastoma. |
| AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID364985 | Antiproliferative activity against PTEN-null human PC3 cells after 96 hrs by alamar blue assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
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| 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. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| The target landscape of clinical kinase drugs. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. |
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| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1798507 | mTOR Assay from Article 10.1021/jm800295d: \\The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinas | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
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| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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
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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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4
| Navigating the kinome. |
| AID1345749 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases) | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1345748 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases) | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1345778 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases) | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1345786 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases) | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |