Assay ID | Title | Year | Journal | Article |
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. |
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. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
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. |
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. |
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. |
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. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
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. |
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. |
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. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1713428 | Hypnotic activity in mouse assessed as onset of sleep time at 0.2 mmol/Kg, ip by righting reflex | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, biological evaluation and molecular modeling study of thiadiazolo[3,2-a][1,3]diazepine analogues of HIE-124 as a new class of short acting hypnotics. |
AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6
| Structure-based identification of OATP1B1/3 inhibitors. |
AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6
| Structure-based identification of OATP1B1/3 inhibitors. |
AID1713422 | Hypnotic activity in mouse assessed as duration of sleep time at 0.2 mmol/Kg, ip by righting reflex | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, biological evaluation and molecular modeling study of thiadiazolo[3,2-a][1,3]diazepine analogues of HIE-124 as a new class of short acting hypnotics. |
AID1713435 | Therapeutic Index, ratio of LD50 of Toxicity in iv dosed mouse to minimum effective hypnotic dose in mouse | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, biological evaluation and molecular modeling study of thiadiazolo[3,2-a][1,3]diazepine analogues of HIE-124 as a new class of short acting hypnotics. |
AID316350 | Hypnotic effect in mouse assessed as sleeping time at 65 mg/kg, ip | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
| New ultra-short acting hypnotic: synthesis, biological evaluation, and metabolic profile of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124). |
AID109886 | Duration of analgesic action in mice was determined; B = brief, < 5 min | 1980 | Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
| Synthesis, biological evaluation, and preliminary structure-activity considerations of a series of alkylphenols as intravenous anesthetic agents. |
AID316340 | Hypnotic effect in mouse assessed as sleeping time at 50 mg/kg, iv by loss of righting reflex method | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
| New ultra-short acting hypnotic: synthesis, biological evaluation, and metabolic profile of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124). |
AID114273 | Hypnotic activity was measured as dose which causes loss of righting reflex for a minimum period of 30s in 50% of mice; Range is 20-25 | 1980 | Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
| Synthesis, biological evaluation, and preliminary structure-activity considerations of a series of alkylphenols as intravenous anesthetic agents. |
AID119873 | Speed of induction of analgesia in mice was determined; I = immediate, <10 s | 1980 | Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
| Synthesis, biological evaluation, and preliminary structure-activity considerations of a series of alkylphenols as intravenous anesthetic agents. |
AID1713434 | Toxicity in iv dosed mouse measured upto 6 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, biological evaluation and molecular modeling study of thiadiazolo[3,2-a][1,3]diazepine analogues of HIE-124 as a new class of short acting hypnotics. |
AID116737 | Acute toxicity measured as median lethal dose in mice; Range is 80-90 | 1980 | Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
| Synthesis, biological evaluation, and preliminary structure-activity considerations of a series of alkylphenols as intravenous anesthetic agents. |
AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11
| 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
AID1129570 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1239424 | Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Development of Selective Covalent Janus Kinase 3 Inhibitors. |
AID1445475 | Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1129579 | Stability of the compound in rat plasma assessed as compound remaining at 50 uM at pH 7.4 after 24 hrs by LC-UV analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1365571 | Inhibition of recombinant human GSt-tagged EGFR T790M/L858R mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system at 10 uM using tyr 04 as substrate after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID748063 | Inhibition of NFkappaB phosphorylation in gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant at 0.01 to 1 uM after 24 hrs by Western blot analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1129581 | GSH reactivity assessed as compound remaining at 50 uM after 1 hr at pH 7.4 by LC-UV analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID662584 | Inhibition of EGFR del E746-A750 mutant in human HCC827 cells assessed as change in EGFR level up to 125 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID775622 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant. |
AID1350816 | Inhibition of TEL-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1583837 | Inhibition of GST-tagged human EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1350815 | Inhibition of TEL-fused EGFR C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1350820 | Inhibition of full length EGFR L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1350830 | Antiproliferative activity against human PC9 cells harboring EGFR del19 mutant after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1241288 | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay | 2015 | Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
| Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach. |
AID552138 | Antiproliferative activity against mouse BA/F3 cells transfected with EGFR L858R/T790M mutant | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID761588 | Inhibition of EGFR phosphorylation in human NCI-H1975 cells assessed as reduction of phosphorylated Akt level at 1 uM after 6 hrs by Western blotting analysis | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID1298672 | Selectivity ratio, ratio IC50 for human A431 cells overexpressing wild-type EGFR to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1445469 | Inhibition of human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 25 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID552139 | Antiproliferative activity against mouse BA/F3 cells transfected with EGFR L858R/T790M/C797S mutant | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1625321 | Selectivity ratio of Kd for wild type partial length human EGFR to Kd for partial length human EGFR L858R/T790M double mutant | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1760611 | Inhibition of recombinant NAMPT (unknown origin) using nicotinamide and pyrophosphate as substrate incubated for 60 mins and measured for 30 mins at 5 mins interval by colorimetric assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer. |
AID1599511 | Inhibition of EGFR (unknown origin) using biotin-labelled peptide as substrate preincubated for 2 hrs followed by substrate addition and measured after 30 mins by HTRF FRET assay | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
| Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors. |
AID1129569 | Inhibition of EGFR L858R/T790M mutant (unknown origin) after 1.5 hr by FRET-based Z-lyte assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1264283 | Antiproliferative activity against human A549 cells harboring wild type EGFR/k-Ras mutation after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID1350835 | Antiproliferative activity against human NCI-H1355 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1458982 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID662508 | Inhibition of EGFR L858R/T790M mutant Y1068 autophosphorylation in human NCI-H1975 cells after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1481348 | Inhibition of Tel-fused INSR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1241286 | Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay | 2015 | Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
| Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach. |
AID662510 | Inhibition of EGFR L858R/T790M mutant-mediated Akt phosphorylation in human NCI-H1975 cells up to 500 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1365579 | Inhibition of ABL in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID1625334 | Potency index, ratio of gefitinib IC50 to compound IC50 for gefitinib resistant mouse BA/F3 cells expressing EGFR L858R/T790M double mutant | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1760612 | Inhibition of N-terminal GST-tagged human recombinant EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer. |
AID770080 | Selectivity ratio of IC50 for wild type EGFR phosphorylation in human LoVo cells over IC50 for EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
AID662512 | Inhibition of EGFR L858R/T790M mutant-mediated Erk phosphorylation in human NCI-H1975 cells up to 500 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1625330 | Antiproliferative activity against gefitinib sensitive mouse BA/F3 cells expressing EGFR exon 19 del E746_A750 activating mutant after 72 hrs by MTS assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID748065 | Inhibition of EGFR L858R/T90M double mutant phosphorylation in gefitinib-resistant human NCI-H1975 cells assessed as inhibition of AKT phosphorylation at 0.01 to 1 uM after 24 hrs by Western blot analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1365567 | Inhibition of recombinant human N-terminal GST/HIS6-tagged EGFR 746 to 750 deletion mutant (672 to 1210 residues) expressed in Sf9 insect cells at 10 uM using tyr 04 as substrate measured after 1 hr by LanthaScreen assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID662596 | Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID775613 | Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells expressing T790M/L858R mutation after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant. |
AID1760614 | Inhibition of N-terminal GST-tagged human recombinant EGFR L861Q mutant (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer. |
AID1390633 | Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA | | | |
AID1365564 | Inhibition of wild-type recombinant human GST-tagged EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system at 1 uM using tyr 04 as substrate measured after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID1129567 | Inhibition of EGFR (unknown origin) after 1.5 hr by FRET-based Z-lyte assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1350829 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID748092 | Cytotoxicity against gefitinib-sensitive human HCC827 cells harboring EGFR E746_A740 deletion mutant assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1625333 | Selectivity ratio of IC50 for gefitinib sensitive mouse BA/F3 cells expressing wild type EGFR to IC50 for gefitinib resistant mouse BA/F3 cells expressing EGFR L858R/T790M double mutant | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID748094 | Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID761598 | Antiproliferative activity against human HCC827 cells expressing EGFR E746_A750 deletion mutant after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID1350831 | Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1129577 | Chemical stability of the compound in buffer solution assessed as compound remaining at 50 uM at pH 7.4 after 24 hrs by LC-UV analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1204630 | Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) T790M/L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay | 2015 | Bioorganic & medicinal chemistry, Jun-15, Volume: 23, Issue:12
| Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR. |
AID748093 | Inhibition of EGFR L858R/T90M double mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID748088 | Cytotoxicity against human A431 cells overexpressing wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1298660 | Inhibition of wild-type EGFR (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1372109 | Selectivity ratio of IC50 for human EGFR T790M mutant to IC50 for human wild type EGFR | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer. |
AID1583838 | Inhibition of GST-tagged human EGFR T790M/L858R double mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID662580 | Inhibition of EGFR del E746-A750 mutant-mediated Erk phosphorylation in human HCC827 cells up to 125 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID748075 | Induction of NO production in human 16HBE14o- cells harboring wild type EGFR assessed as increase in nitrite level at 100 uM after 150 mins by Griess assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID748087 | Cytotoxicity against human BEAS2B cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1365573 | Inhibition of recombinant human GST-tagged EGFR C797S mutant cytoplasmic domain (695 to end residues) expressed in insect cells at 10 uM using tyr 04 measured after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID552134 | Inhibition of Jak2 transfected with TEL fusion in mouse BA/F3 cells | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1365580 | Inhibition of ABL T315I mutant in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID662588 | Inhibition of EGFR del E746-A750 mutant in human HCC827 cells assessed as change in Akt level up to 125 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1470861 | Antiproliferative activity against non-special gene type human HT-29 cells after 48 hrs by SRB assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
| Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle. |
AID1458979 | Selectivity ratio of IC50 for wild type N-terminal GST-fused human EGFR cytoplasmic domain to IC50 for human recombinant GST-tagged EGFR L858R/T790M double mutant | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1760613 | Inhibition of N-terminal GST-tagged human recombinant EGFR T790M mutant (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer. |
AID1715791 | Inhibition of recombinant human N-terminal GST tagged EGFR L858R mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID662582 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as change in EGFR level up to 500 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID761600 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID662590 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as change in Erk level up to 500 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1298661 | Inhibition of EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID748064 | Inhibition of EGFR L858R/T90M double mutant phosphorylation in gefitinib-resistant human NCI-H1975 cells assessed as inhibition of ERK phosphorylation at 0.01 to 1 uM after 24 hrs by Western blot analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1129568 | Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hr by FRET-based Z-lyte assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1458984 | Selectivity ratio of EC50 for human A431 cells expressing wild type EGFR to EC50 for human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1129583 | L-cysteine reactivity assessed as compound remaining at 50 uM after 1 hr at pH 7.4 by LC-UV analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID662592 | Inhibition of EGFR del E746-A750 mutant in human HCC827 cells assessed as change in Erk level up to 125 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1445470 | Inhibition of human N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 20 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1350838 | Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID662483 | Binding affinity to EGFR | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1264284 | Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID748072 | Induction of apoptosis in gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant after 24 hrs by annexin-V/7-AAD staining-based FACS flow cytometric analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1583841 | Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID748070 | Induction of apoptosis in EGFR-independent human H460 cells at 1 to 5 uM after 24 hrs by annexin-V/7-AAD staining-based FACS flow cytometric analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1481311 | Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1583842 | Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1239473 | Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Development of Selective Covalent Janus Kinase 3 Inhibitors. |
AID1483368 | Inhibition of EGFR L858R mutant (unknown origin) | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
AID1129572 | Antiproliferative activity against human A431 cells overexpressing WT EGFR after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID770083 | Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
AID662598 | Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1458977 | Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 15 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1760615 | Inhibition of N-terminal GST-tagged human recombinant EGFR L858R mutant (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer. |
AID1350813 | Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1483369 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
AID1264286 | Inhibition of human recombinant EGFR T790M/L858R double mutant preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID1845553 | Inhibition of N-terminal GST-tagged wild type human NUAK1 expressed in Escherichia coli DH5alpha incubated for 30 mins in presence of gamma-[32P]ATP by cerenkov counting analysis | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development and Therapeutic Potential of NUAKs Inhibitors. |
AID1350821 | Inhibition of full length EGFR L858R/T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID748086 | Cytotoxicity against human 16HBE14o- cells harboring wild type EGFR assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1583845 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1625320 | Binding affinity to partial length human EGFR L858R/T790M double mutant expressed in mammalian system by KINOMEscan assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID552132 | Antiproliferative activity against EGFR-deficient human PC9 cells | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID748089 | Cytotoxicity against human A549 cells harboring wild type EGFR and k-RAS mutation assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID748071 | Induction of apoptosis in gefitinib-sensitive human HCC827 cells harboring EGFR E746_A740 deletion mutant after 24 hrs by annexin-V/7-AAD staining-based FACS flow cytometric analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID552135 | Inhibition of Jak3 transfected with TEL fusion in mouse BA/F3 cells | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1129578 | Chemical stability of the compound in buffer solution assessed as compound remaining at 50 uM at pH 9 after 24 hrs by LC-UV analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1708306 | Antiproliferative activity against human NCI-H1975 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1625319 | Binding affinity to wild type partial length human EGFR expressed in bacterial system by KINOMEscan assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1470862 | Selectivity index, ratio of IC50 for human A549 cells harboring wild type EGFR to IC50 for human NCI-H1975 cells harboring EGFR L858R/T790M double mutant | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
| Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle. |
AID1365577 | Inhibition of EGFR E746_A750 deletion/T790M mutant in human growth-resistant PC9 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID552141 | Antiproliferative activity against mouse BA/F3 cells transfected with EGFR E746_A750_del/T790M/C797S mutant | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1298671 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1715789 | Inhibition of recombinant human N-terminal GST tagged EGFR L858R/T790M double mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by T | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1239474 | Antiproliferative activity against mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Development of Selective Covalent Janus Kinase 3 Inhibitors. |
AID775624 | Inhibition of wild type EGFR (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant. |
AID1583844 | Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1458981 | Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID662600 | Antiproliferative activity against human HL7702 cells expressing wilt type EGFR after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID662480 | Inhibition of EGFR L858R mutant after 1.5 hr by FRET assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1390636 | Inhibition of recombinant human GST-tagged EGFR L858R/T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay | | | |
AID1390635 | Inhibition of recombinant human GST-tagged wild-type EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay | | | |
AID662481 | Inhibition of EGFR L861Q mutant after 1.5 hr by FRET assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1239472 | Binding affinity to JAK3 (unknown origin) | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Development of Selective Covalent Janus Kinase 3 Inhibitors. |
AID1625328 | Antiproliferative activity against gefitinib resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1129574 | Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1390641 | Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay | | | |
AID1365566 | Inhibition of recombinant human N-terminal GST/HIS6-tagged EGFR 746 to 750 deletion mutant (672 to 1210 residues) expressed in Sf9 insect cells at 1 uM using tyr 04 as substrate measured after 1 hr by LanthaScreen assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID770081 | Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
AID1583843 | Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID748090 | Cytotoxicity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID662478 | Inhibition of EGFR after 1.5 hr by FRET assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1129582 | DTT reactivity assessed as compound remaining at 50 uM after 1 hr at pH 7.4 by LC-UV analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1350834 | Antiproliferative activity against human NCI-H2122 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1365568 | Inhibition of recombinant human GST-tagged EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system at 1 uM using tyr 04 as substrate after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID552140 | Antiproliferative activity against mouse BA/F3 cells transfected with EGFR E746_A750_del/T790M mutant | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1129575 | Antiproliferative activity against human 16HBE cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1483367 | Inhibition of wild-type EGFR (unknown origin) | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
AID1350832 | Antiproliferative activity against human H3255 cells harboring EGFR L858R mutant after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1129573 | Antiproliferative activity against k-RAS dependent human A549 cells overexpressing WT EGFR after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1365578 | Inhibition of EGFR in human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID662599 | Antiproliferative activity against human A549 cells expressing wild type EGFR coexpressing k-Ras mutant after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID552136 | Inhibition of Blk transfected with TEL fusion in mouse BA/F3 cells | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1625324 | Selectivity ratio of IC50 for human A431 cells expressing wild type EGFR to IC50 for human NCI-H1975 cells expressing EGFR L858R/T790M double mutant | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1470859 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 48 hrs by SRB assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
| Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle. |
AID770082 | Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
AID748091 | Inhibition of wild type EGFR (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID761596 | Antiproliferative activity against human 16HBE cells expressing wild type EGFR after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID748060 | Antitumor activity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant xenografted in athymic BALB/c nude mouse assessed as tumor growth inhibition at 8 mg/kg, ip qd administered for 14 days measured every other day d | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1204628 | Inhibition of wild type N-terminal His6-tagged human EGFR kinase domain (702 to 1016 residues) expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay | 2015 | Bioorganic & medicinal chemistry, Jun-15, Volume: 23, Issue:12
| Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR. |
AID1673938 | Growth inhibition of human HN11 cells harboring wild type EGFR after 72 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1483366 | Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
| Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
AID1715790 | Inhibition of recombinant human N-terminal GST tagged EGFR d746-750 mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET ass | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1625331 | Antiproliferative activity against mouse BA/F3 cells expressing wild type EGFR after 72 hrs by MTS assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID748066 | Inhibition of EGFR L858R/T90M double mutant phosphorylation in gefitinib-resistant human NCI-H1975 cells at 0.01 to 1 uM after 24 hrs by Western blot analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1365569 | Inhibition of recombinant human GST-tagged EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system at 10 uM using tyr 04 as substrate after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID552133 | Antiproliferative activity against growth-resistant human PC9 cells expressing EGFR E746_A750/T790M mutant | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1350817 | Inhibition of full length EGFR del19 mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID719892 | Binding affinity to recombinant EGFR L858R/T90M mutant | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Irreversible protein kinase inhibitors: balancing the benefits and risks. |
AID1583836 | Inhibition of wild type GST-tagged human EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1445476 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1365575 | Inhibition of recombinant human GST-tagged EGFR C797S L858R mutant cytoplasmic domain (695 to end residues) expressed in insect cells at 10 uM using tyr 04 measured after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID662509 | Inhibition of EGFR del E746-A750 mutant Y1068 autophosphorylation in human HCC827 cells after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1264285 | Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID761602 | Inhibition of EGFR L858R mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID1458983 | Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1390638 | Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA | | | |
AID1458980 | Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1298670 | Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1365576 | Inhibition of EGFR E746_A750 deletion mutant in human PC9 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID1599557 | Inhibition of cathepsin C (unknown origin) | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
| Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors. |
AID1264289 | Inhibition of wild type recombinant human EGFR preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID775623 | Inhibition of EGFR L858R mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant. |
AID1264287 | Inhibition of human recombinant EGFR T790M/delE746_A750 double mutant preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID662578 | Inhibition of EGFR del E746-A750 mutant-mediated Akt phosphorylation in human HCC827 cells up to 125 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID761587 | Inhibition of EGFR phosphorylation in human NCI-H1975 cells assessed as reduction of phosphorylated Erk level at 1 uM after 6 hrs by Western blotting analysis | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID748076 | Induction of NO production in human NCI-H1975 cells harboring EGFR L858R/T90M double mutant assessed as increase in nitrite level at 100 uM after 150 mins by Griess assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1481349 | Inhibition of Tel-fused IGF1R (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1625332 | Antiproliferative activity against gefitinib resistant human PC9 cells expressing EGFR del E746_A750/T790M mutant after 72 hrs by MTS assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1599510 | Inhibition of CatL-activated recombinant human C-terminal His10-tagged cathepsin C (25 to 463 residues) expressed in mouse myeloma cells using Gly-Phe-AFC as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
| Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors. |
AID1241287 | Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay | 2015 | Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
| Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach. |
AID552137 | Inhibition of Bmx transfected with TEL fusion in mouse BA/F3 cells | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1458976 | Inhibition of wild type N-terminal GST-fused human EGFR cytoplasmic domain expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 25 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1390640 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay | | | |
AID1129571 | Antiproliferative activity against gefitinib-sensitive human HCC827 cells bearing EGFR del E746_A750 mutant after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID761603 | Inhibition of wild type EGFR (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID1625329 | Antiproliferative activity against gefitinib resistant mouse BA/F3 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTS assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1625323 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant by MTS assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID761601 | Inhibition of EGFR L858R/T790M mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID1204629 | Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay | 2015 | Bioorganic & medicinal chemistry, Jun-15, Volume: 23, Issue:12
| Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR. |
AID1708231 | Antiproliferative activity against human PC-9 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1264290 | Selectivity ratio of IC50 for human recombinant EGFR T790M/L858R double mutant to IC50 for wild type recombinant human EGFR | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID775614 | Antiproliferative activity against gefitinib-sensitive human HCC827 cells harboring EGFR E746 to A750 deletion after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant. |
AID662586 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as change in Akt level up to 500 nM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID662597 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1470860 | Antiproliferative activity against human A549 cells harboring wild type EGFR after 48 hrs by SRB assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
| Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle. |
AID761597 | Antiproliferative activity against human A431 cells expressing wild type EGFR after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID662482 | Inhibition of EGFR L858R/T790M mutant after 1.5 hr by FRET assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1350839 | Antiproliferative activity against CHL cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1583835 | Inhibition of GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID662485 | Binding affinity to EGFR L858R mutant | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1365574 | Inhibition of recombinant human GST-tagged EGFR C797S L858R mutant cytoplasmic domain (695 to end residues) expressed in insect cells at 1 uM using tyr 04 measured after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID1350822 | Inhibition of full length EGFR L858R/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1264288 | Inhibition of human recombinant EGFR T790M mutant preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID1365565 | Inhibition of wild-type recombinant human GST-tagged EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system at 10 uM using tyr 04 as substrate measured after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID552142 | Antiproliferative activity against mouse BA/F3 cells transfected with EGFR E746_A750/T790M mutant | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of selective irreversible inhibitors for EGFR-T790M. |
AID1445477 | Inhibition of human EGFR T790M/C797S/L858R triple mutant preincubated for 20 mins followed by [33P]ATP addition measured after 2 hrs | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1350814 | Inhibition of TEL-fused EGFR (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1673937 | Growth inhibition of human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1583840 | Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID662479 | Inhibition of EGFR T790M mutant after 1.5 hr by FRET assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1365572 | Inhibition of recombinant human GST-tagged EGFR C797S mutant cytoplasmic domain (695 to end residues) expressed in insect cells at 1 uM using tyr 04 measured after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID761589 | Inhibition of EGFR phosphorylation in human NCI-H1975 cells at 0.01 to 1 uM after 6 hrs by Western blotting analysis | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID1625335 | Potency index, ratio of gefitinib IC50 to compound IC50 for gefitinib resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID1583839 | Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1298662 | Selectivity index, ratio IC50 for wild-type EGFR (unknown origin) expressed in baculovirus expression system to IC50 for EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
| Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1445468 | Inhibition of human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 15 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID761599 | Antiproliferative activity against wild type EGFR/k-Ras dependent human A549 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID1350833 | Antiproliferative activity against human A549 cells harboring wild-type EGFR after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
AID1625322 | Antiproliferative activity against human A431 cells expressing wild type EGFR by MTS assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
AID662601 | Ratio of WZ4002 IC50 to compound IC50 for human NCI-H1975 cells | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1365570 | Inhibition of recombinant human GSt-tagged EGFR T790M/L858R mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system at 1 uM using tyr 04 as substrate after 1 hr by Z'-LYTE assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID1458978 | Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 20 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
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. |
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. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
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. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
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. |
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. |
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. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
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. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
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. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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. |
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. |
AID1345741 | Human NUAK family kinase 1 (NuaK subfamily) | 2009 | Nature, Dec-24, Volume: 462, Issue:7276
| Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. |
AID1345572 | Human erb-b2 receptor tyrosine kinase 4 (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2009 | Nature, Dec-24, Volume: 462, Issue:7276
| Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. |
AID1345705 | Human IL2 inducible T cell kinase (Tec family) | 2009 | Nature, Dec-24, Volume: 462, Issue:7276
| Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. |
AID1345682 | Human BLK proto-oncogene, Src family tyrosine kinase (Src family) | 2009 | Nature, Dec-24, Volume: 462, Issue:7276
| Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. |
AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2009 | Nature, Dec-24, Volume: 462, Issue:7276
| Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. |
AID1345617 | Human Bruton tyrosine kinase (Tec family) | 2009 | Nature, Dec-24, Volume: 462, Issue:7276
| Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |