| Assay ID | Title | Year | Journal | Article |
|---|
| AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1879279 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G2/M phase at 25 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12.8 to 13.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID507584 | Binding affinity to KIT V559D,V654A mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID526668 | Binding affinity to RET | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
| AID1369897 | Inhibition of FLT3 ITD mutant autophosphorylation at Y842 in human MV4-11 cells at 1 nM after 1 hr by immunoblot analysis | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1879267 | Inhibition of CDK2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1360811 | Induction of apoptosis in human MV4-11 cells assessed as live cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1540763 | Inhibition of human VEGFR2 using poly[Glu:Tyr] (4:1) substrate and [gamma-33P]-ATP by radiometric biochemical kinase assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID508141 | AUC (0 to 24 hrs) in nu/nu mouse at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508112 | Binding affinity to TLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507883 | Binding affinity to CSNK1A1L | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508120 | Binding affinity to TSSK1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507606 | Binding affinity to MAPKAPK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1369865 | Growth inhibition of human K562 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID507815 | Binding affinity to ABL1 Q252H mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438525 | Half life in Sprague-Dawley rat at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1152834 | Inhibition of FLT3 kinase (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
| Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors. |
| AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476247 | Tmax in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424973 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1779476 | Antiproliferative activity against human MV4-11 cells harbouring FLT-ITD mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID508079 | Binding affinity to RPS6KA5(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507833 | Binding affinity to ARK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507884 | Binding affinity to CSNK1D | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507593 | Binding affinity to LYN | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425061 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507922 | Binding affinity to EPHA4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424894 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1587559 | Toxicity in NOD/SCID mouse xenografted with human MOLM13 cells at 3 mg/kg, po qd for 10 days | | | |
| AID507667 | Binding affinity to PDPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691316 | Cytotoxicity against human KG-1a cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1906352 | Induction of apoptosis in human MV4-11 cells assessed as accumulation of annexin-V positive cells measured after 24 to 48 hrs by AnnexinV-FITC/PI staining based flow cytometry analysis | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1587448 | Inhibition of FLT3 autophosphorylation in human MV4-11 cells assessed as ratio of phosphorylated FLT3 to beta-actin level at 3 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID508123 | Binding affinity to TYK2(JH1domain-catalytic) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476264 | Binding affinity to RET (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1476263 | Binding affinity to PDGFRbeta (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1476256 | Oral bioavailability in Sprague-Dawley rat at 10 mg/mg | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1691317 | Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID507955 | Binding affinity to FLT3 ITD mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1906338 | Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1476273 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-D835V mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508082 | Binding affinity to SBK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879269 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as reduction in STAT3 phosphorylation at Y694 residue at 5 to 25 nM measured after 1 hr by immunoblotting analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID507612 | Binding affinity to MEK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507957 | Binding affinity to FLT3 N841I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1635664 | Toxicity in nude BALB/c mouse assessed as body weight change at 10 to 25 mg/kg, po qd for 14 days measured every 2 days | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1635686 | Binding affinity to FLT3 ITD/F691L mutant (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID508137 | Binding affinity to ZAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508147 | Antitumor activity against human MV4-11 cells xenografted mouse model assessed as inhibition of tumor regrowth at at 10 mg/kg, po 60 days post treatment | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1676246 | Inhibition of FLT3 ITD mutant (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
| Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507840 | Binding affinity to BIKE | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507911 | Binding affinity to EGFR G719S mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1691315 | Cytotoxicity against human KG-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507925 | Binding affinity to EPHA7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369876 | Growth inhibition of human BJ cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1691322 | Cytotoxicity against human PL21 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508061 | Binding affinity to RET V804M mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438524 | Clearance in Sprague-Dawley rat at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369867 | Inhibition of N-terminal GST/His6-fused recombinant human FLT3 (R571 to S993 residues) D835Y mutant expressed in Sf9 insect cells using poly (Ala,Glu,Lys,Tyr) 6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507646 | Binding affinity to NEK6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1305301 | Competitive inhibition of FLT3 D835Y mutant (unknown origin) in presence of ATP | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5
| Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. |
| AID1587452 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as ratio of phosphorylated STAT5 to beta-actin level at 3 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID438535 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 3 mg/kg, po QD for 28 days measured after 21 days postdose | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507891 | Binding affinity to CTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508093 | Binding affinity to SRPK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425084 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507976 | Binding affinity to IGF1R | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1661764 | Binding affinity to recombinant human FLT3 ITD mutant expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID507853 | Binding affinity to CAMK1D | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508081 | Binding affinity to RPS6KA6(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508087 | Binding affinity to SLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508043 | Binding affinity to PRKCD | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507632 | Binding affinity to MST1R | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507897 | Binding affinity to DCAMKL3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508153 | Inhibition of FLT3 autophosphorylation in human AML cells isolated from relapsed acute myeloid leukemia patient by Western blotting | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1777272 | Inhibition of CDK2/Cyclin A1 (unknown origin) at 1 uM using histone H1 as substrate preincubated for 20 mins followed by 33P-ATP addition and measured after 2 hrs by filter binding method | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| 3 |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425129 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508067 | Binding affinity to RIPK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507594 | Binding affinity to LZK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507947 | Binding affinity to FGFR3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1771734 | Antiproliferative activity against human MOLM-14 cells harboring FLT3-ITD mutant assessed as cell growth inhibition by resazurin assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor. |
| AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438511 | Binding affinity to PDGFRbeta | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1661775 | Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID507973 | Binding affinity to HPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1676247 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
| Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. |
| AID1587430 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835V mutant measured after 72 hrs by MTT assay | | | |
| AID1764683 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 4 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1369866 | Inhibition of N-terminal GST/His6-fused recombinant wild type human FLT3 (R571 to S993 residues) expressed in Sf9 insect cells using poly (Ala,Glu,Lys,Tyr) 6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1425169 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508074 | Binding affinity to RPS6KA2(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507890 | Binding affinity to CSNK2A2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507856 | Binding affinity to CAMK2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508035 | Binding affinity to PKAC-beta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507828 | Binding affinity to AKT3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369870 | Growth inhibition of human THP1 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507913 | Binding affinity to EGFR L747-S752del, P753S mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508070 | Binding affinity to ROS1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID674406 | Antiproliferative activity against human MOLM13 cells expressing FLT3-ITD mutant | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
| AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507564 | Binding affinity to IKK-alpha | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507604 | Binding affinity to MAP4K5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507810 | Binding affinity to ABL1 E255K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508155 | Inhibition of FLT3 ITD mutant autophosphorylation in human blast cells after 2 hrs by electrochemiluminescence | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764684 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 1 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1779475 | Antiproliferative activity against mouse Ba/F3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1587446 | Inhibition of FLT3 autophosphorylation in human MV4-11 cells assessed as ratio of phosphorylated FLT3 to beta-actin level at 10 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID1369879 | Growth inhibition of mouse BA/F3 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID508062 | Binding affinity to RIOK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1691335 | Cytotoxicity against human NB-4 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1779472 | Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 D835Y mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID1476242 | AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1424948 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508108 | Binding affinity to TGFBR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508118 | Binding affinity to TRKB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507966 | Binding affinity to GSK3A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1691333 | Cytotoxicity against human MONO-MAC-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID507892 | Binding affinity to DAPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508040 | Binding affinity to PLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507838 | Binding affinity to AURKC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1691313 | Cytotoxicity against human EOL1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID507933 | Binding affinity to ERBB3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1540824 | Induction of apoptosis in human MOLM14 cells at 1 uM incubated for 24 hrs by propidium iodide and annexin-V staining based flow cytometry | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID507965 | Binding affinity to GRK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476262 | Binding affinity to PDGFRalpha (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507814 | Binding affinity to ABL1 M351T mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID674404 | Inhibition of VEGFR2 | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
| AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507908 | Binding affinity to EGFR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508056 | Binding affinity to QSK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1369931 | In vivo inhibition of FLT3 ITD mutant in human MV4-11 cells xenografted in athymic nu/nu mouse assessed as decrease in STAT5 phosphorylation at Y694 at 10 mg/kg, ip after 24 hrs by immunoblot method relative to control | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1476274 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835Y mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507887 | Binding affinity to CSNK1G2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508071 | Binding affinity to RPS6KA1(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507945 | Binding affinity to FGFR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507617 | Binding affinity to MELK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507645 | Binding affinity to NEK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1518691 | Inhibition of wildtype FLT3 (unknown origin) using TAMRA-Src-tide as substrate measured after 1 hr in presence of ATP at its Km concentration by IMAP-FP assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507871 | Binding affinity to CDKL2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1691295 | Cytotoxicity against human IM-9 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID508140 | Tmax in nu/nu mouse at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507822 | Binding affinity to ACVR2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508132 | Binding affinity to YANK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1305302 | Competitive inhibition of FLT3 ITD mutant (unknown origin) in presence of ATP | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5
| Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. |
| AID1360800 | Inhibition of FLT3 in human MV4-11 cells assessed as reduction in STAT5 phosphorylation at Tyr694 residue at 0.1 uM after 4 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID438528 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 1 mg/kg, po QD for 28 days measured after dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1879274 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G1 phase at 5 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 57.9 to 59.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID507938 | Binding affinity to ERK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1779471 | Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD D835Y mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID507967 | Binding affinity to GSK3B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507835 | Binding affinity to ASK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476298 | Antiproliferative activity against human CMK cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507951 | Binding affinity to FLT1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691329 | Cytotoxicity against human U-266 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1906334 | Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1691330 | Cytotoxicity against human KMOE-2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1434661 | Growth inhibition of FLT3 null human K562 cells by CCK8 assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C |
| AID1906344 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424952 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1518686 | Inhibition of human partial length FLT3 ITD mutant expressed in bacterial expression system by Kinomescan method | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507603 | Binding affinity to MAP4K4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625081 | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1187150 | Growth inhibition of human MV411 cells after 48 hrs by XTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents. |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425080 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476254 | MRT (0 to infinity) in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507855 | Binding affinity to CAMK2A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1540761 | Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID1540762 | Inhibition of TEL-fused VEGFR3 (unknown origin) expressed in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID438510 | Binding affinity to PDGFRalpha | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID438513 | Binding affinity to CSF1R | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1476297 | Antiproliferative activity against human HL60 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1661820 | Half life in Wistar rat at 3 mg/kg, po measured upto 24 hrs by UPLC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID508145 | In vivo inhibition of FLT3 autophosphorylation in human MV4-11 cells xenografted in mouse at 10 mg/kg, po after 2 hrs | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507936 | Binding affinity to ERK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507895 | Binding affinity to DCAMKL1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424941 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1587463 | Inhibition of FLT3 autophosphorylation in human MOLM13 cells assessed as ratio of phosphorylated FLT3 to beta-actin level at 10 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1779474 | Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD F691I mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID507601 | Binding affinity to MAP4K2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1369872 | Growth inhibition of human MCF7 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1425109 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1540766 | Inhibition of TEL-fused FLT3 (unknown origin) expressed in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507589 | Binding affinity to LIMK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1518696 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID438516 | Binding affinity to DDR1 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1424959 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507870 | Binding affinity to CDK9 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508024 | Binding affinity to PIK3CA Q546K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507889 | Binding affinity to CSNK2A1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508078 | Binding affinity to RPS6KA5(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID438522 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1777273 | Inhibition of human FLT3 ITD mutant using EAIYAAPFAKKK as substrate preincubated for 20 mins followed by 33P-ATP addition and measured after 2 hrs by filter binding method | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| 3 |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507905 | Binding affinity to DYRK1A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508058 | Binding affinity to RET | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764688 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 37 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508049 | Binding affinity to PRKD3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1879281 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at S phase at 125 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 27.7 to 28.6%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1518698 | Cytotoxicity against human HS5 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID507677 | Binding affinity to PIK3CA E545A mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507880 | Binding affinity to CLK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507673 | Binding affinity to PIK3C2G | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507847 | Binding affinity to BRAF V600E mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1587445 | Antitumour activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as tumour growth inhibition at 3 mg/kg, po qd for 18 days measured every two days during compound dosing by caliper method relative to control | | | |
| AID508091 | Binding affinity to SRPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508089 | Binding affinity to SRC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425074 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507819 | Binding affinity to ACVR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507888 | Binding affinity to CSNK1G3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879263 | Antiproliferative activity against human Kasumi 1 cells harboring N822K KIT mutant | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476240 | AUC (0 to t) in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507829 | Binding affinity to ALK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476289 | Antiproliferative activity against TEL-fused PDGFRbeta-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508115 | Binding affinity to TNK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508037 | Binding affinity to PKN1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508113 | Binding affinity to TNIK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507648 | Binding affinity to NEK9 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1906336 | Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1906360 | Antitumor activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 1 mg/kg,po qd measured after 28 days by caliper method | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID508142 | Oral bioavailability in rat at 3 mg/kg | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507577 | Binding affinity to JNK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424931 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507946 | Binding affinity to FGFR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1369900 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in MEK1/2 phosphorylation at S217/221 at 0.01 to 100 nM after 1 hr by immunoblot analysis | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1476244 | Cmax in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1476255 | MRT (0 to infinity) in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1691320 | Cytotoxicity against human OCI-AML2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1476202 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-D835Y mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1187153 | Inhibition of human FLT D835Y mutant using 10 uM ATP | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents. |
| AID438529 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as tumor growth regression at 3 mg/kg, po QD for 28 days measured after dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1424968 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425072 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507611 | Binding affinity to MAST1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691323 | Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1187152 | Growth inhibition of human THP1 cells after 48 hrs by XTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents. |
| AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476276 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835N mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1234689 | Inhibition of wild type BCR/ABL in FLT3 deficient human K562 cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID508084 | Binding affinity to SgK110 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508094 | Binding affinity to STK16 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1906346 | Cytotoxicity in human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1476338 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at G0/G1 phase at 100 nM after 12 hrs by propidium iodide staining based-FACS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1424983 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508057 | Binding affinity to RAF1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476296 | Antiproliferative activity against human OCI-AML2 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369898 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in STAT5 phosphorylation at Y694 at 0.01 to 100 nM after 1 hr by immunoblot analysis | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507961 | Binding affinity to GAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476272 | Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FLT3 kinase after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587458 | Inhibition of MAPK in human MV4-11 cells assessed as ratio of phosphorylated ERK to beta-actin level at 10 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID438507 | Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1587471 | Inhibition of MAPK in human MOLM13 cells assessed as ratio of phosphorylated ERK to beta-actin level at 1 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507959 | Binding affinity to FRK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476252 | Apparent clearance in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1737428 | Inhibition of FLT3 autophosphorylation in human RS4-11 cells preincubated for 2 hrs followed by FLT3 ligand addition and measured after 15 mins | | | |
| AID1696916 | Inhibition of FLT3 ITD mutant (unknown origin) expressed in mouse BaF3 cells | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508092 | Binding affinity to SRPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507878 | Binding affinity to CLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508126 | Binding affinity to ULK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1635586 | Antiproliferative activity against FLT3-deficient human K562 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID508122 | Binding affinity to TXK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1235146 | Inhibition of human FLT3 at 100 nM incubated for 40 mins using EAIYAAPFAKKK substrate and [gamma-33P-ATP] by scintillation counting method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Discovery of novel N-(5-(tert-butyl)isoxazol-3-yl)-N'-phenylurea analogs as potent FLT3 inhibitors and evaluation of their activity against acute myeloid leukemia in vitro and in vivo. |
| AID507633 | Binding affinity to MST2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1879268 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as reduction in autophosphorylation at Y589/591 residue at 5 to 25 nM measured after 1 hr by immunoblotting analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1779470 | Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID508100 | Binding affinity to TAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691300 | Binding affinity to human partial length FLT3 ITD/F691L double mutant expressed in mammalian expression system by Kinomescan method | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1661777 | Cytotoxicity against human KG1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1906339 | Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369874 | Growth inhibition of human MRC5 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID507975 | Binding affinity to ICK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476268 | Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1476266 | Binding affinity to CSF1R (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1317472 | Inhibition of recombinant human FLT3 expressed in insect Sf21 cells preincubated for 15 mins followed by poly(Glu:Tyr) substrate addition for 30 mins in presence of [gamma-32P]ATP by TR-FRET assay | 2016 | European journal of medicinal chemistry, Sep-14, Volume: 120 | Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia. |
| AID507588 | Binding affinity to LIMK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507954 | Binding affinity to FLT3 D835Y mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1234790 | Antitumor activity against mouse 32D cells expressing FLT3 ITD D835Y mutant allografted in nude mouse assessed as tumor growth inhibition at 10 mg/kg/day, po administered 5 days on/2 days off schedule for 4 weeks relative to vehicle-treated control | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1906348 | Inhibition of FLT3 ITD mutant (unknown orgin) by ADP-glo kinase assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID507872 | Binding affinity to CDKL3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508121 | Binding affinity to TTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1777274 | Antiproliferative activity against human K562 cells assessed as cell death measured after 72 hrs by resazurin dye based assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| 3 |
| AID507909 | Binding affinity to EGFR E746-A750del mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507599 | Binding affinity to MAP3K3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507861 | Binding affinity to CAMKK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1878086 | Inhibition of FLT3-ITD autophosphorylation in human MV4-11 cells measured after 2 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID1424994 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1661779 | Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508026 | Binding affinity to PIK3CD | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476267 | Binding affinity to FLT1 (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507634 | Binding affinity to MST3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507972 | Binding affinity to HIPK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369899 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in ERK1/2 phosphorylation at T202/Y204 at 0.01 to 100 nM after 1 hr by immunoblot analysis | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID674403 | Inhibition of VEGFR1 | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507802 | Toxicity in human MV4-11 cells xenografted mouse bone marrow engraftment model assessed as body weight loss at 10 mg/kg/day, po for 30 days | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425009 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507902 | Binding affinity to DMPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508154 | Cytotoxicity against human AML cells isolated from relapsed acute myeloid leukemia patient harboring FLT3 ITD mutation by MTT assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID526666 | Binding affinity to PDGFRalpha | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
| AID507654 | Binding affinity to p38-delta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1360813 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1518692 | Inhibition of FLT3 ITD mutant (unknown origin) using TAMRA-Src-tide as substrate measured after 1 hr in presence of ATP at its Km concentration by IMAP-FP assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID1234784 | Antitumor activity against human MV4-11 cells xenografted in nude mouse assessed as tumor regression at 10 mg/kg, po qd administered on day 1 to 5 measured during 48 days post last dose | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID507597 | Binding affinity to MAP3K15 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1234683 | Inhibition of recombinant GST-tagged VEGFR2 kinase domain (V789 to V1356) (unknown origin) expressed in insect Sf9 cells using polyGlu4:Tyr peptide as substrate after 120 mins by Kinase-Glo assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID507963 | Binding affinity to GRK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507574 | Binding affinity to JH1 catalytic domain JAK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476275 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835I mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507943 | Binding affinity to FER | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508151 | Antitumor activity against human MV4-11 cells xenografted mouse bone marrow engraftment model assessed as increase mouse life span at 1 mg/kg/day, po for 30 days measured on day 77 post dose | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1234682 | Inhibition of wild type GST-tagged FLT3 kinase domain (Y567 to S993) (unknown origin) expressed in baculovirus infected insect Sf9 cells using Her2 peptide as substrate after 4 hrs by Kinase-Glo assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1696919 | Cytotoxicity against mouse BaF3 cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations. |
| AID508031 | Binding affinity to PIM3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1545697 | Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID507580 | Binding affinity to KIT D816V mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1635661 | Antitumor activity against human MV4-11 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 10 mg/kg, po qd for 14 days measured every 2 days | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1360799 | Inhibition of FLT3 phosphorylation at Tyr589/591 residues in human MV4-11 cells at 0.1 uM after 4 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1906333 | Cytotoxicity in phyto-hematoagglutinin induced human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1540765 | Inhibition of human VEGFR3 using poly[Glu:Tyr] (4:1) substrate and [gamma-33P]-ATP by radiometric biochemical kinase assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID507804 | Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507610 | Binding affinity to MARK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508125 | Binding affinity to TYRO3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507595 | Binding affinity to MAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507570 | Binding affinity to IRAK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1234767 | Inhibition of drug resistant human FLT3 ITD D835F mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1661760 | Inhibition of FLT3 ITD mutant expressed in human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1635587 | Antiproliferative activity against human WI38 cells after 72 hrs by SRB assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1764687 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 111 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1878085 | Inhibition of FLT3 autophosphorylation in human RS4-11 cells measured after 2 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID1434660 | Inhibition of N-terminal GST-tagged recombinant human wild-type FLT3 (564 to end residues) D835Y mutant expressed in baculovirus infected sf21 cells using Abltide as substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C |
| AID1540826 | Induction of apoptosis in human MV4-11 cells at 1 uM incubated for 24 hrs by propidium iodide and annexin-V staining based flow cytometry | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID507623 | Binding affinity to MKNK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507915 | Binding affinity to EGFR L858R mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID438518 | Cmax in athymic nude mouse at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1661758 | Inhibition of FLT3 ITD mutant expressed in human BaF3 cells assessed as reduction in cell growth incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507676 | Binding affinity to PIK3CA E542K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1852969 | Inhibition of FLT3-ITD mutant in human MV4-11 cells assessed as decrease in FLT3 protein level at 0.03 to 3 uM incubated for 24 hrs by Western blot analysis | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12
| Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein. |
| AID1879276 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G2/M phase at 5 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12.8 to 13.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID508097 | Binding affinity to STK36 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1434662 | Growth inhibition of human THP1 cells harboring wild-type FLT3 by XTT assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C |
| AID507628 | Binding affinity to MLK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1369880 | Selectivity ratio of IC50 for N-terminal GST/His6-fused recombinant human FLT3 (R571 to S993 residues) D835Y mutant to IC50 for N-terminal GST/His6-fused recombinant human FLT3 (R571 to S993 residues) ITD mutant | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1587472 | Inhibition of MAPK in human MOLM13 cells assessed as ratio of phosphorylated ERK to beta-actin level at 3 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID1587428 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutant measured after 72 hrs by MTT assay | | | |
| AID507827 | Binding affinity to AKT2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508039 | Binding affinity to PLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438536 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 10 mg/kg, po QD for 28 days measured after 32 days postdose | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508129 | Binding affinity to VEGFR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1434658 | Inhibition of N-terminal GST-tagged recombinant human wild-type FLT3 (564 to end residues) expressed in baculovirus infected sf21 cells assessed as residual activity at 1 uM using Abltide as substrate in presence of [gamma33P]ATP after 10 mins by scintill | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C |
| AID507830 | Binding affinity to AMPK-alpha1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425088 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508066 | Binding affinity to RIPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1430636 | Inhibition of human TrkC at 500 nM using poly[Glu:Tyr] (4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 2 hrs by Hotspot assay | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach. |
| AID1587461 | Inhibition of FLT3 autophosphorylation in human MOLM13 cells assessed as ratio of phosphorylated FLT3 to beta-actin level at 1 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587482 | Antitumour activity against human MOLM13 cells xenografted in NOD/SCID mouse assessed as tumour growth inibition at 3 mg/kg, po qd for 10 days measured every two days during compound dosing by caliper method relative to control | | | |
| AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508136 | Binding affinity to YSK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508051 | Binding affinity to PRKG2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438515 | Binding affinity to FLT4 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID508052 | Binding affinity to PRKR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507952 | Binding affinity to FLT3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1602341 | Binding affinity to human FLT3 ITD/D835V double mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID507653 | Binding affinity to p38-beta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1852975 | Inhibition of STAT5 phosphorylation in human MV4-11 cells at 0.03 to 3 uM incubated for 24 hrs by Western blot analysis | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12
| Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein. |
| AID508103 | Binding affinity to TAOK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1545695 | Cytotoxicity against FIP1L1-PDGFRA positive human EOL-1 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1234685 | Inhibition of FLT3 ITD heterozygous mutant in human MOLM-13 cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID507670 | Binding affinity to PHKG1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507934 | Binding affinity to ERBB4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476225 | Inhibition of human HL60 cells-derived His-tagged FLT3 (564 to 993 residues) expressed in baculovirus infected sf9 cells using poly (4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo kinase assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1425107 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508034 | Binding affinity to PKAC-alpha | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID438531 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as suppression of tumor volume at 3 mg/kg, po QD for 28 days measured after dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476322 | Induction of apoptosis in human MOLM14 cells assessed as cleavage of PARP at 100 nM after 24 hrs by immunoblotting method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507583 | Binding affinity to KIT V559D,T670I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508095 | Binding affinity to STK33 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1602343 | Binding affinity to non-auto-inhibited form of wild type human N-terminal GST-tagged FLT3 expressed in baculovirus expression | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476260 | Binding affinity to DDR2 (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508102 | Binding affinity to TAOK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587560 | Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells at 3 mg/kg, po qd for 18 days | | | |
| AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1369863 | Inhibition of N-terminal GST/His6-fused recombinant human FLT3 (R571 to S993 residues) ITD mutant expressed in Sf9 insect cells using poly (Ala,Glu,Lys,Tyr) 6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID507953 | Binding affinity to FLT3 D835H mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507858 | Binding affinity to CAMK2G | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507912 | Binding affinity to EGFR L747-E749del, A750P mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507568 | Binding affinity to INSRR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507948 | Binding affinity to FGFR3 G697C mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507839 | Binding affinity to AXL | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425096 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507585 | Binding affinity to LATS1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1906343 | Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID507590 | Binding affinity to LKB1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425095 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507672 | Binding affinity to PIK3C2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438517 | Binding affinity to VEGFR2 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID507818 | Binding affinity to ABL2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508065 | Binding affinity to RIPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1896657 | Binding affinity to RIPK1 (unknown origin) | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
| Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities. |
| AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476291 | Antiproliferative activity against human MOLM13 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1764682 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 12 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1879264 | Antiproliferative activity against human K562 cells | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1476243 | AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1369864 | Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID507569 | Binding affinity to IRAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1369896 | Inhibition of FLT3 ITD mutant autophosphorylation at Y589/591 in human MV4-11 cells at 1 nM after 1 hr by immunoblot analysis | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1602342 | Binding affinity to human FLT3 ITD/F691L double mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID1764690 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 4 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1430641 | Inhibition of FLT3-ITD mutant-driven human MOLM14 cell proliferation after 72 hrs by alamar blue assay | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach. |
| AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476265 | Binding affinity to KIT (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508054 | Binding affinity to PRP4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507841 | Binding affinity to BLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507605 | Binding affinity to MAPKAPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508080 | Binding affinity to RPS6KA6(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507625 | Binding affinity to MLCK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507939 | Binding affinity to ERK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879273 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G2/M phase at 1 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12.8 to 13.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1518697 | Antiproliferative activity against human U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID1430640 | Inhibition of FLT3-ITD mutant-driven human MV4-11 cell proliferation after 72 hrs by alamar blue assay | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach. |
| AID507616 | Binding affinity to MEK6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507944 | Binding affinity to FES | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508098 | Binding affinity to STK39 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1906351 | Induction of apoptosis in human MV4-11 cells assessed as accumulation of annexin-V positive cells at 1 to 50 nM by AnnexinV-FITC/PI staining based flow cytometry analysis | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID508088 | Binding affinity to SNARK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507901 | Binding affinity to DMPK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1830543 | Inhibition of FLT3 (unknown origin) using Poly (Glu,Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. |
| AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1879278 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at S phase at 25 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 27.7 to 28.6%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1360801 | Inhibition of FLT3 in human MV4-11 cells assessed as reduction in AKT phosphorylation at Ser473 residue at 0.1 uM after 4 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID507596 | Binding affinity to MAP3K1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1691293 | Cytotoxicity against human OCI-M1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID507910 | Binding affinity to EGFR G719C mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508127 | Binding affinity to ULK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425189 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507579 | Binding affinity to KIT | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879272 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at S phase at 1 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 27.7 to 28.6%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID507647 | Binding affinity to NEK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507576 | Binding affinity to JNK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507874 | Binding affinity to CHEK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424984 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507614 | Binding affinity to MEK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508138 | Binding affinity to ZAP70 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507600 | Binding affinity to MAP3K4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507626 | Binding affinity to MLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1906345 | Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1737410 | Antiproliferative activity against human MOLM14 cells harboring ITD/F691L mutant assessed as cell growth inhibition by MTT assay | | | |
| AID1317474 | Growth inhibition of human K562 cells after 48 hrs by XTT assay | 2016 | European journal of medicinal chemistry, Sep-14, Volume: 120 | Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia. |
| AID507649 | Binding affinity to NIM1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1830542 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. |
| AID1476277 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835G mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID438540 | Ratio of tandutinib IC50 to compound IC50 for human MV4-11 cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507940 | Binding affinity to ERK8 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425038 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508027 | Binding affinity to PIK3CG | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507886 | Binding affinity to CSNK1G1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507586 | Binding affinity to LATS2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424937 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507821 | Binding affinity to ACVR2A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508106 | Binding affinity to TESK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508131 | Binding affinity to WEE2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507657 | Binding affinity to PAK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507826 | Binding affinity to AKT1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476280 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-D835H mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507816 | Binding affinity to ABL1 T315I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508047 | Binding affinity to PRKD1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1779473 | Antiproliferative activity against mouse Ba/F3 cells harbouring FLT3 ITD F691L mutant assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID507969 | Binding affinity to HIPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764680 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 111 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507619 | Binding affinity to MET | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508048 | Binding affinity to PRKD2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507639 | Binding affinity to MYO3A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507968 | Binding affinity to HCK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425172 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1661770 | Binding affinity to recombinant human RET (713 to 1014 residues) expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1369873 | Growth inhibition of human HCC827 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476241 | AUC (0 to t) in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1879270 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as reduction in ERK1/2 phosphorylation at T202/Y204 residue at 5 to 25 nM measured after 1 hr by immunoblotting analysis | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID507929 | Binding affinity to EPHB3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1360812 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1906340 | Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1317476 | Growth inhibition of human HL60 cells expressing wild type FLT-3 after 48 hrs by XTT assay | 2016 | European journal of medicinal chemistry, Sep-14, Volume: 120 | Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia. |
| AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507881 | Binding affinity to CSF1R | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1830544 | Inhibition of FLT3-ITD mutant (unknown origin) using Poly (Glu,Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. |
| AID507885 | Binding affinity to CSNK1E | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507820 | Binding affinity to ACVR1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1830545 | Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507661 | Binding affinity to PAK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507807 | Toxicity against human A375 cells after 72 hrs by cell titer-blue assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438512 | Binding affinity to RET | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID507644 | Binding affinity to NEK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425020 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508124 | Binding affinity to TYK2(JH2domain-pseudokinase) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507651 | Binding affinity to OSR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1661772 | Selectivity index, ratio of Kd for recombinant human KIT (571 to 972 residues) expressed in bacterial expression system to Kd for recombinant human FLT3 ITD mutant expressed in bacterial expression system | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1691338 | Cytotoxicity against human TF-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID507573 | Binding affinity to JAK1 JH2 domain | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID438539 | Toxicity in athymic nude mouse xenografted with human MV4-11 cells assessed as body weight loss at 1 to 10 mg/kg, po QD for 28 days measured after 32 days postdose | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1635585 | Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425054 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1691318 | Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID508042 | Binding affinity to PLK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476248 | Half life in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID438526 | Bioavailability in Sprague-Dawley rat at 10 mg/kg | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1424918 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1661759 | Cytotoxicity against human BAF3 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID526667 | Binding affinity to PDGFRbeta | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
| AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438508 | Binding affinity to Kit | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID507844 | Binding affinity to BMPR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507960 | Binding affinity to FYN | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587468 | Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as ratio of phosphorylated STAT5 to beta-actin level at 10 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID1476293 | Antiproliferative activity against human U937 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1369930 | In vivo inhibition of FLT3 ITD mutant autophosphorylation at Y589/592 in human MV4-11 cells xenografted in athymic nu/nu mouse at 10 mg/kg, ip after 2 to 48 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764685 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 1000 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1425090 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425015 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507875 | Binding affinity to CHEK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1540767 | Growth inhibition of mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID507664 | Binding affinity to PCTK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587466 | Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as ratio of phosphorylated STAT5 to beta-actin level at 1 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1201287 | Inhibition of FLT3 (unknown origin) using FAM-EPLYWSFPA as substrate preincubated for 60 mins followed by substrate addition by microfluidics assay in presence of 190 uM ATP | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors. |
| AID1852974 | Inhibition of FLT3 phosphorylation in human MV4-11 cells at 0.03 to 3 uM incubated for 24 hrs by Western blot analysis | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12
| Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein. |
| AID1545699 | Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID507671 | Binding affinity to PHKG2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID438520 | AUC (0 to infinity) in athymic nude mouse at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID507575 | Binding affinity to JH1 catalytic domain of JAK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508150 | Antitumor activity against human MV4-11 cells xenografted mouse bone marrow engraftment model assessed as increase mouse life span at 10 mg/kg/day, po for 30 days measured on day 172 post dose | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424936 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507638 | Binding affinity to MYLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507669 | Binding affinity to PFTK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507637 | Binding affinity to MYLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425212 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424906 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507941 | Binding affinity to ERN1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507652 | Binding affinity to p38-alpha | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1234765 | Inhibition of drug resistant human FLT3 ITD D835Y mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587429 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-F691L mutant measured after 72 hrs by MTT assay | | | |
| AID1425132 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425158 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476259 | Binding affinity to DDR1 (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507581 | Binding affinity to KIT L576P mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507970 | Binding affinity to HIPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507624 | Binding affinity to MKNK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507571 | Binding affinity to ITK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476286 | Antiproliferative activity against TEL-fused cKIT-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1737408 | Antiproliferative activity against human MOLM14 cells harboring ITD mutant assessed as cell growth inhibition by MTT assay | | | |
| AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507920 | Binding affinity to EPHA2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1434657 | Growth inhibition of human HL60 cells harboring wild-type FLT3 by CCK8 assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C |
| AID507817 | Binding affinity to ABL1 Y253F mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1661776 | Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1661771 | Selectivity index, ratio of Kd for recombinant human CSF1R (564 to 939 residues) expressed in bacterial expression system to Kd for recombinant human FLT3 ITD mutant expressed in bacterial expression system | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID508073 | Binding affinity to RPS6KA2(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507927 | Binding affinity to EPHB1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879265 | Inhibition of FLT3 ITD mutant (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1764653 | Selectivity ratio of IC50 for c-KIT (unknown orign) to IC50 for FLT3 (unknown origin) | | | |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508086 | Binding affinity to SIK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507917 | Binding affinity to EGFR L861Q mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507831 | Binding affinity to AMPK-alpha2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508099 | Binding affinity to SYK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1234687 | Cytotoxicity against FLT3-deficient human U937 cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1187149 | Growth inhibition of human K562 cells after 48 hrs by XTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507635 | Binding affinity to MST4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424932 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508053 | Binding affinity to PRKX | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879280 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G1 phase at 125 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 57.9 to 59.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508023 | Binding affinity to PIK3CA M1043I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507931 | Binding affinity to EPHB6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507859 | Binding affinity to CAMK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507906 | Binding affinity to DYRK1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587451 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as ratio of phosphorylated STAT5 to beta-actin level at 1 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID507640 | Binding affinity to MYO3B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507849 | Binding affinity to BRSK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507823 | Binding affinity to ACVRL1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424972 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1777276 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 100 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 59.6%) | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| 3 |
| AID507866 | Binding affinity to CDK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507850 | Binding affinity to BRSK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508085 | Binding affinity to SIK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425034 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507578 | Binding affinity to JNK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507832 | Binding affinity to ANKK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476283 | Antiproliferative activity against TEL-fused DDR1-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507659 | Binding affinity to PAK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507813 | Binding affinity to ABL1 H396P mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507873 | Binding affinity to CDKL5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507894 | Binding affinity to DAPK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425207 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508063 | Binding affinity to RIOK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507658 | Binding affinity to PAK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476287 | Antiproliferative activity against TEL-fused LCK-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507930 | Binding affinity to EPHB4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476294 | Antiproliferative activity against human SKM1 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508033 | Binding affinity to PIP5K2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507865 | Binding affinity to CDK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438532 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as suppression of tumor volume at 10 mg/kg, po QD for 28 days measured after dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1879262 | Antiproliferative activity against human EOL1 cells expressing IP1L1-PDGFRA fusion protein | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507643 | Binding affinity to NEK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476316 | Cell cycle arrest in human MOLM14 cells assessed as accumulation at G0/G1 phase at 100 nM after 12 hrs by propidium iodide staining based-FACS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1879277 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G1 phase at 25 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 57.9 to 59.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1764686 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 333 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1476246 | Tmax in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507674 | Binding affinity to PIK3CA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1635583 | Inhibition of FLT3 (unknown origin) (592 to 969 residues) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507974 | Binding affinity to HUNK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508128 | Binding affinity to ULK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1777275 | Antiproliferative activity against human MV4-11 cells assessed as cell death measured after 72 hrs by resazurin dye based assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| 3 |
| AID1187148 | Inhibition of human FLT3 using 10 uM ATP | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents. |
| AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1691314 | Cytotoxicity against human HL-60 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425042 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1430637 | Inhibition of human c-Kit at 500 nM using poly[Glu:Tyr] (4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 2 hrs by Hotspot assay | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach. |
| AID507675 | Binding affinity to PIK3CA C420R mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1771735 | Antiproliferative activity against human MOLM-14 cells harboring FLT3-ITD D835Y mutant assessed as cell growth inhibition by resazurin assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor. |
| AID507962 | Binding affinity to GCN2 Kin.Dom.2, S808G mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1737409 | Antiproliferative activity against human MOLM14 cells harboring ITD/D835Y mutant assessed as cell growth inhibition by MTT assay | | | |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1635687 | Binding affinity to auto-inhibited FLT3 (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID438342 | Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1879261 | Antiproliferative activity against human MV4-11 cells expressing FLT3-ITD mutant | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID625058 | Binding constant for VRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507803 | Binding affinity to FLT3 catalytic domain by KinomeScan kinase binding assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425122 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507592 | Binding affinity to LTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1661766 | Binding affinity to recombinant human FLT3 ITD/F691L double mutant expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508149 | Antitumor activity against human MV4-11 cells xenografted mouse bone marrow engraftment model assessed as increase in mouse survival at 10 mg/kg/day, po for 30 days | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508044 | Binding affinity to PRKCE | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507622 | Binding affinity to MINK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1635685 | Binding affinity to FLT3 ITD/D835V mutant (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1518695 | Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507668 | Binding affinity to PFTAIRE2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1430638 | Inhibition of human FLT3 at 500 nM using EAIYAAPFAKKK as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 2 hrs by Hotspot assay relative to control | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach. |
| AID438519 | Tmax in athymic nude mouse at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1852971 | Inhibition of FLT3-ITD mutant in human MV4-11 cells assessed as decrease in AXL protein level at 0.03 to 3 uM incubated for 24 hrs by Western blot analysis | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12
| Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein. |
| AID507916 | Binding affinity to EGFR L858R,T790M mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507845 | Binding affinity to BMX | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1635684 | Binding affinity to FLT3 D835V mutant (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID674402 | Inhibition of wild type FLT3 | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
| AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507848 | Binding affinity to BRK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507800 | Toxicity in human MV4-11 cells xenografted mouse bone marrow engraftment model assessed as toxic incidences at 10 mg/kg/day, po for 30 days | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476253 | Apparent clearance in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507932 | Binding affinity to ERBB2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1691325 | Cytotoxicity against human L-363 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1476278 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835A mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1187151 | Growth inhibition of human HL60 cells after 48 hrs by XTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents. |
| AID1661761 | Inhibition of recombinant human N-terminal GST/His6-tagged FLT3 ITD mutant (571 to 993 residues) expressed in Sf9 cells using Tyr2 peptide as substrate incubated for 1.5 hrs by Z'-LYTE assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508022 | Binding affinity to PIK3CA H1047Y mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508041 | Binding affinity to PLK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879282 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G2/M phase at 125 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12.8 to 13.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID507582 | Binding affinity to KIT V559D mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508050 | Binding affinity to PRKG1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476292 | Antiproliferative activity against human MOLM14 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507919 | Binding affinity to EPHA1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507587 | Binding affinity to LCK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691337 | Cytotoxicity against human SKM-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424986 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424925 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508083 | Binding affinity to SgK085 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507630 | Binding affinity to MRCKB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507907 | Binding affinity to DYRK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1545701 | Selectivity index, ratio of GI50 for human BJ cells to GI50 for FIP1L1-PDGFRA positive human EOL-1 cells after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID507857 | Binding affinity to CAMK2D | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476281 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-K663Q mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507860 | Binding affinity to CAMKK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508059 | Binding affinity to RET M918T mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID438523 | AUC in Sprague-Dawley rat at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1425211 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507811 | Binding affinity to ABL1 F317I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508069 | Binding affinity to ROCK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1691298 | Inhibition of human FLT3 ITD mutant EAIYAAPFAKKK peptide as substrate in presence of 33P-gamma ATP by hotspot kinase assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1771736 | Antiproliferative activity against human MOLM-14 cells harboring FLT3-ITD F691L mutant assessed as cell growth inhibition by resazurin assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor. |
| AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424975 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1764679 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 1000 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507854 | Binding affinity to CAMK1G | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476279 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835del mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1635680 | Binding affinity to wild type FLT3 (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1661773 | Selectivity index, ratio of Kd for recombinant human PDGFRA (575 to 1002 residues) expressed in mammalian expression system to Kd for recombinant human FLT3 ITD mutant expressed in bacterial expression system | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507918 | Binding affinity to EGFR S752-I759del mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507928 | Binding affinity to EPHB2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508046 | Binding affinity to PRKCQ | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508109 | Binding affinity to TIE1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476321 | Induction of apoptosis in human MOLM13 cells assessed as cleavage of PARP at 100 nM after 12 hrs by immunoblotting method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369934 | In vivo inhibition of FLT3 ITD mutant in human MV4-11 cells xenografted in athymic nu/nu mouse assessed as decrease in ERK1/2 phosphorylation at T202/Y204 at 10 mg/kg, ip after 24 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508064 | Binding affinity to RIOK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425005 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507950 | Binding affinity to FGR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476328 | Induction of apoptosis in human MOLM14 cells assessed as cleavage of caspase-3 at 100 nM after 24 hrs by immunoblotting method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508075 | Binding affinity to RPS6KA3(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507621 | Binding affinity to MET Y1235D mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1234787 | Antitumor activity against human MOLM13 cells xenografted in SCID mouse assessed as increase in survival at 10 mg/kg, po qd administered on day 1 to 5 and day 8 to 12 relative to vehicle-treated control | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1518685 | Inhibition of wild-type human partial length FLT3 (V592 to Y969 residues) expressed in bacterial expression system by Kinomescan method | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507608 | Binding affinity to MARK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587467 | Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as ratio of phosphorylated STAT5 to beta-actin level at 3 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1369901 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in AKT phosphorylation at S473 at 0.01 to 100 nM after 1 hr by immunoblot analysis | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507893 | Binding affinity to DAPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507958 | Binding affinity to FLT4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1635681 | Binding affinity to FLT3 ITD mutant (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1661768 | Binding affinity to recombinant human PDGFRA (575 to 1002 residues) expressed in mammalian expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1906347 | Inhibition of wild type FLT3 (unknown origin) by ADP-glo kinase assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID507864 | Binding affinity to CDK11 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425167 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507678 | Binding affinity to PIK3CA E545K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507808 | Binding affinity to AAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID526669 | Binding affinity to CSF1R | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
| AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425137 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507650 | Binding affinity to NLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507921 | Binding affinity to EPHA3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1369932 | In vivo inhibition of FLT3 ITD mutant in human MV4-11 cells xenografted in athymic nu/nu mouse assessed as decrease in STAT5 phosphorylation at Y694 at 10 mg/kg, ip after 48 hrs by immunoblot method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1696917 | Inhibition of FLT3 ITD/D835Y double mutant (unknown origin) expressed in mouse BaF3 cells | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations. |
| AID1691334 | Cytotoxicity against human MONO-MAC-6 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508148 | Toxicity in human MV4-11 cells xenografted mouse model assessed as change in body weight at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476282 | Antiproliferative activity against TEL-fused CSF1R-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507655 | Binding affinity to p38-gamma | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507867 | Binding affinity to CDK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507896 | Binding affinity to DCAMKL2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1661765 | Binding affinity to recombinant human FLT3 ITD/D835V double mutant expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587456 | Inhibition of MAPK in human MV4-11 cells assessed as ratio of phosphorylated ERK to beta-actin level at 1 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID1602339 | Binding affinity to human FLT3 D835H mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID507565 | Binding affinity to IKK-beta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476257 | Antitumor activity against human MV4-11 cells harboring FLT3-ITD mutation xenografted in nu/nu mouse assessed as tumor growth inhibition at 10 mg/kg/day, po administered via gavage every day for 28 days relative to control | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508076 | Binding affinity to RPS6KA4(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507620 | Binding affinity to MET M1250T mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507679 | Binding affinity to PIK3CA H1047L mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507876 | Binding affinity to CIT | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425079 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424987 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476226 | Inhibition of human MV4-11 cells-derived His-tagged FLT3 ITD mutant (564 to 993 residues) expressed in baculovirus infected sf9 cells using poly (4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo kinase assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID507914 | Binding affinity to EGFR L747-T751del, Sins mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1234786 | Antitumor activity against human MV4-11 cells xenografted in nude mouse assessed as tumor regression at 10 mg/kg, po qd administered on day 8 to 12 measured during 48 days post last dose | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1425099 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507666 | Binding affinity to PDGFRB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID438514 | Binding affinity to FLT1 | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID507607 | Binding affinity to MARK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425154 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508119 | Binding affinity to TRKC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508072 | Binding affinity to RPS6KA1(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508152 | Antitumor activity against human MV4-11 cells xenografted mouse bone marrow engraftment model assessed as increase mouse life span at 0.1 mg/kg/day, po for 30 days | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424945 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1234684 | Inhibition of recombinant GST-tagged Aurora-A kinase domain (S123 to S401) (unknown origin) expressed in insect Sf9 cells using tetra(LRRASLG) peptide as substrate after 90 mins by Kinase-Glo assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1425010 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624981 | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507665 | Binding affinity to PDGFRA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425100 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507824 | Binding affinity to ADCK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1737407 | Antiproliferative activity against wild type human MOLM14 cells assessed as cell growth inhibition by MTT assay | | | |
| AID1906335 | Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476290 | Antiproliferative activity against TEL-fused RET-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508110 | Binding affinity to TIE2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691336 | Cytotoxicity against human OCI-AML5 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID508096 | Binding affinity to STK35 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507862 | Binding affinity to CDC2L1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508030 | Binding affinity to PIM2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1830546 | Inhibition of FLT3 D835Y mutant (unknown origin) using Poly (Glu,Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. |
| AID508135 | Binding affinity to YSK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507572 | Binding affinity to JH1 catalytic domain JAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507956 | Binding affinity to FLT3 K663Q mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438521 | Half life in athymic nude mouse at 10 mg/kg, po | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508134 | Binding affinity to YES | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1906337 | Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1476245 | Cmax in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1317473 | Inhibition of human FLT3 D835Y mutant preincubated for 15 mins followed by poly(Glu:Tyr) substrate addition for 30 mins in presence of [gamma-32P]ATP by TR-FRET assay | 2016 | European journal of medicinal chemistry, Sep-14, Volume: 120 | Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia. |
| AID1635682 | Binding affinity to FLT3 D835H mutant (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507971 | Binding affinity to HIPK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507806 | Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507863 | Binding affinity to CDC2L2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1434663 | Growth inhibition of human MV4-11 cells harboring FLT3-ITD mutant by XTT assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587425 | Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant measured after 72 hrs by MTT assay | | | |
| AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507964 | Binding affinity to GRK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507923 | Binding affinity to EPHA5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507904 | Binding affinity to DRAK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507825 | Binding affinity to ADCK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID438527 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 1 mg/kg, po QD for 28 days measured during dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1696918 | Inhibition of FLT3 ITD/F691L double mutant (unknown origin) expressed in mouse BaF3 cells | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations. |
| AID507660 | Binding affinity to PAK6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507662 | Binding affinity to PCTK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587457 | Inhibition of MAPK in human MV4-11 cells assessed as ratio of phosphorylated ERK to beta-actin level at 3 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1764781 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 333 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID507879 | Binding affinity to CLK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1879266 | Inhibition of PDGFRalpha (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID507843 | Binding affinity to BMPR1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507900 | Binding affinity to DLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507834 | Binding affinity to ASK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507869 | Binding affinity to CDK8 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764681 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 37 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID624986 | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507851 | Binding affinity to BTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476269 | Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1691327 | Cytotoxicity against human OPM-2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587562 | Antitumour activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as tumour growth inhibition at 10 mg/kg, po qd for 18 days measured on day 26 by caliper method | | | |
| AID507924 | Binding affinity to EPHA6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1661763 | Binding affinity to recombinant human FLT3 (592 to 969 residues) expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1476284 | Antiproliferative activity against TEL-fused DDR2-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1661767 | Binding affinity to recombinant human KIT (571 to 972 residues) expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID508107 | Binding affinity to TGFBR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507636 | Binding affinity to MUSK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507882 | Binding affinity to CSK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1661762 | Binding affinity to recombinant human CSF1R (564 to 939 residues) expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476250 | Apparent volume of distribution in Sprague-Dawley rat at 1 mg/mg, iv | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508036 | Binding affinity to PKMYT1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507846 | Binding affinity to BRAF | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438530 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as tumor growth regression at 10 mg/kg, po QD for 28 days measured after dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425115 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476329 | Induction of apoptosis in human MV4-11 cells assessed as cleavage of caspase-3 at 100 nM after 48 hrs by immunoblotting method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1234766 | Inhibition of drug resistant human FLT3 ITD D835V mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508111 | Binding affinity to TLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507898 | Binding affinity to DDR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1360814 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID1587447 | Inhibition of FLT3 autophosphorylation in human MV4-11 cells assessed as ratio of phosphorylated FLT3 to beta-actin level at 1 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1587462 | Inhibition of FLT3 autophosphorylation in human MOLM13 cells assessed as ratio of phosphorylated FLT3 to beta-actin level at 3 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507615 | Binding affinity to MEK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507937 | Binding affinity to ERK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476285 | Antiproliferative activity against TEL-fused FLT4-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1234686 | Inhibition of FLT3 ITD homozygous mutant in human MV4-11 cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507631 | Binding affinity to MST1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1779484 | Inhibition of FAK in human MDA-MB-231 cells assessed as inhibition of paxillin phosphorylation at 0.5 to 5 uM incubated for 24 hrs by Western blot analysis | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Identification of Thieno[3,2- |
| AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507837 | Binding affinity to AURKB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507602 | Binding affinity to MAP4K3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1234688 | Inhibition of wild type homozygous FLT3 in human RS4:11 cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID1369869 | Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476295 | Antiproliferative activity against human NB4 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507627 | Binding affinity to MLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508032 | Binding affinity to PIP5K1A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1360802 | Inhibition of FLT3 in human MV4-11 cells assessed as reduction in ERK1/2 phosphorylation at Thr202/Tyr204 residues at 0.1 uM after 4 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Discovery of the selective and efficacious inhibitors of FLT3 mutations. |
| AID507642 | Binding affinity to NDR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1661774 | Selectivity index, ratio of Kd for recombinant human RET (713 to 1014 residues) expressed in bacterial expression system to Kd for recombinant human FLT3 ITD mutant expressed in bacterial expression system | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507598 | Binding affinity to MAP3K2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508060 | Binding affinity to RET(V804L) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508114 | Binding affinity to TNK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508077 | Binding affinity to RPS6KA4(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587453 | Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as ratio of phosphorylated STAT5 to beta-actin level at 10 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507935 | Binding affinity to ERK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507567 | Binding affinity to INSR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587427 | Inhibition of recombinant human FLT3 (564 to end residues) using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma-33P]-ATP by scintillation counting analysis | | | |
| AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424915 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1676245 | Inhibition of FLT3 ITD mutant (unknown origin) at 500 nM relative to control | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
| Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. |
| AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507949 | Binding affinity to FGFR4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508133 | Binding affinity to YANK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476288 | Antiproliferative activity against TEL-fused PDGFRalpha-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1691339 | Cytotoxicity against human MOLP-2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507877 | Binding affinity to CLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1476317 | Cell cycle arrest in human MOLM13 cells assessed as accumulation at G0/G1 phase at 100 nM after 12 hrs by propidium iodide staining based-FACS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1879275 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at S phase at 5 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 27.7 to 28.6%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1369933 | In vivo inhibition of FLT3 ITD mutant in human MV4-11 cells xenografted in athymic nu/nu mouse assessed as decrease in ERK1/2 phosphorylation at T202/Y204 at 10 mg/kg, ip after 2 hrs by immunoblot method relative to control | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507852 | Binding affinity to CAMK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508055 | Binding affinity to PYK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1878049 | Anticancer activity against human MV4-11 cells expressing homozygous AML-FLT3-ITD assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID508028 | Binding affinity to PIK4CB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508045 | Binding affinity to PRKCH | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691299 | Inhibition of human FLT3 D835Y mutant EAIYAAPFAKKK peptide as substrate in presence of 33P-gamma ATP by hotspot kinase assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1234768 | Inhibition of drug resistant human FLT3 ITD F691L mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508139 | Cmax in nu/nu mouse at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508144 | In vivo inhibition of FLT3 autophosphorylation in human MV4-11 cells xenografted in mouse at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508104 | Binding affinity to TBK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1235145 | Cytotoxicity against human MV4-11 cells incubated for 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Discovery of novel N-(5-(tert-butyl)isoxazol-3-yl)-N'-phenylurea analogs as potent FLT3 inhibitors and evaluation of their activity against acute myeloid leukemia in vitro and in vivo. |
| AID507809 | Binding affinity to ABL1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1369868 | Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID507805 | Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508025 | Binding affinity to PIK3CB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508130 | Binding affinity to WEE1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1602340 | Binding affinity to human FLT3 ITD mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID1587426 | Antiproliferative activity against human MOLM13 cells harboring FLT3-ITD mutant measured after 72 hrs by MTT assay | | | |
| AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1879271 | Cell cycle arrest in human MV4-11 cells expressing FLT3-ITD mutant assessed as accumulation at G1 phase at 1 nM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 57.9 to 59.5%) | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors. |
| AID1906342 | Antiproliferative activity against human PL21 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1878048 | Anticancer activity against human MOLM-13 cells expressing heterogenous AML-FLT3-ITD assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476271 | Antiproliferative activity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1545696 | Inhibition of recombinant human 3C cleavage site/N-terminal GST-His6 fused PDGFR alpha C-terminal fragment (Q551 to L1089 residues) harboring V561D mutant expressed in baculovirus infected Sf9 insect cells using AGLT peptide as substrate in presence of [g | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476327 | Induction of apoptosis in human MOLM13 cells assessed as cleavage of caspase-3 at 100 nM after 12 hrs by immunoblotting method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1317477 | Growth inhibition of human MV4-11 cells expressing FLT3-ITD after 48 hrs by XTT assay | 2016 | European journal of medicinal chemistry, Sep-14, Volume: 120 | Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia. |
| AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1691331 | Cytotoxicity against human ME-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1369875 | Growth inhibition of HUVEC after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1691328 | Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691332 | Cytotoxicity against human ML-2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507629 | Binding affinity to MRCKA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424914 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507899 | Binding affinity to DDR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507868 | Binding affinity to CDK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424899 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476323 | Induction of apoptosis in human MV4-11 cells assessed as cleavage of PARP at 100 nM after 48 hrs by immunoblotting method | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508090 | Binding affinity to SRMS | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507842 | Binding affinity to BMPR1A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587473 | Inhibition of MAPK in human MOLM13 cells assessed as ratio of phosphorylated ERK to beta-actin level at 10 nM after 2 hrs by Western blot analysis relative to control | | | |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507656 | Binding affinity to PAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1369878 | Inhibition of FLT3 ITD mutant (unknown origin) transfected in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID1691319 | Cytotoxicity against human NOMO-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1540764 | Inhibition of human FLT3 using EAIYAAPFAKKK substrate and [gamma-33P]-ATP by radiometric biochemical kinase assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
| Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508105 | Binding affinity to TEC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1545698 | Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508038 | Binding affinity to PKN2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507618 | Binding affinity to MERTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID526664 | Binding affinity to FLT3 | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
| AID507903 | Binding affinity to DRAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1518693 | Inhibition of FLT3 D835Y (unknown origin) using TAMRA-Src-tide as substrate measured after 1 hr in presence of ATP at its Km concentration by IMAP-FP assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1906341 | Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. |
| AID507613 | Binding affinity to MEK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507591 | Binding affinity to LOK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1476251 | Apparent volume of distribution in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID1635683 | Binding affinity to FLT3 D835Y mutant (unknown origin) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants. |
| AID1661778 | Cytotoxicity against human NB4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID1234764 | Inhibition of human FLT3 ITD mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
| AID507566 | Binding affinity to IKK-epsilon | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508068 | Binding affinity to ROCK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476261 | Binding affinity to FLT4 (unknown origin) by KinomeSCan assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508101 | Binding affinity to TAO1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1476249 | Half life in Sprague-Dawley rat at 10 mg/mg, po | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutan |
| AID508116 | Binding affinity to TNNI3K | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508146 | In vivo inhibition of FLT3 autophosphorylation in human MV4-11 cells xenografted in mouse at 10 mg/kg, po after 24 hrs | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID674405 | Inhibition of Aurora A | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
| AID507812 | Binding affinity to ABL1 F317L mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1545700 | Cytotoxicity against human BJ cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1434659 | Inhibition of N-terminal GST-tagged recombinant human wild-type FLT3 (564 to end residues) expressed in baculovirus infected sf21 cells using Abltide as substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C |
| AID1317475 | Growth inhibition of human THP1 cells expressing wild type FLT-3 after 48 hrs by XTT assay | 2016 | European journal of medicinal chemistry, Sep-14, Volume: 120 | Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia. |
| AID507836 | Binding affinity to AURKA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1661769 | Binding affinity to recombinant human PDGFRB (582 to 1009 residues) expressed in bacterial expression system by Kinomescan method | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508117 | Binding affinity to TRKA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424927 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507663 | Binding affinity to PCTK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1425073 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507926 | Binding affinity to EPHA8 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508029 | Binding affinity to PIM1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507942 | Binding affinity to FAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1369871 | Growth inhibition of human U937 cells after 72 hrs by calcein AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Discovery of N |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764691 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 1 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID526665 | Binding affinity to cKIT | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
| AID507609 | Binding affinity to MARK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764689 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 12 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507641 | Binding affinity to NDR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
| Highly predictive and interpretable models for PAMPA permeability. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1
| Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
| 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. |
| 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. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
| Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| 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. |
| AID1345503 | Human fms related tyrosine kinase 3 (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1345563 | Human platelet derived growth factor receptor alpha (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1345590 | Human platelet derived growth factor receptor beta (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1345503 | Human fms related tyrosine kinase 3 (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1345914 | Human ret proto-oncogene (Type XIV RTKs: RET) | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1345503 | Human fms related tyrosine kinase 3 (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1345508 | Human colony stimulating factor 1 receptor (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1345555 | Human KIT proto-oncogene receptor tyrosine kinase (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |