| Assay ID | Title | Year | Journal | Article |
|---|
| AID1880041 | Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| AID1718003 | Selectivity ratio of IC50 for antiproliferative activity against human Rh41 cells to IC50 for inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1617963 | Antiproliferative activity against human HCC827 cells assessed as inhibition of cell growth at 10 uM incubated for 48 hrs by MTT assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1416438 | Inhibition of phosphorylated FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1584404 | Antiproliferative activity against FGF19/FGFR4 expressing human HuH7 cells after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1880028 | Inhibition of FGFR2 N549H mutant (unknown origin) by radiometric kinase activity assay | | | |
| AID1416439 | Inhibition of phosphorylated FGFR1 (407 to 822 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1880036 | Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| AID1880030 | Inhibition of FGFR3 K650M mutant (unknown origin) by radiometric kinase activity assay | | | |
| AID1880022 | Inhibition of wild-type FGFR2 (unknown origin) by radiometric kinase activity assay | | | |
| AID1880120 | Inhibition of CYP2D6 (unknown origin) assessed as remaining activity at 10 uM relative to control | | | |
| AID1778525 | Inhibition of FGFR2 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1458777 | Inhibition of SMO V404M mutant in gefitinib resistant human HCC827 cells assessed as decrease in GLI1 activity by GLI1 luciferase reporter assay | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. |
| AID1717995 | Antiproliferative activity against human Rh41 cells assessed as reduction in cell viability measured after 3 days | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880034 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| AID1778527 | Inhibition of FGFR4 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1431259 | Inhibition of recombinant GST fused FGFR3 (unknown origin) using poly(EY) 4:1 as substrate in presence of [gamma-32P]ATP after 10 mins by scintillation counting method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1717961 | Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability by cell proliferation assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880029 | Inhibition of FGFR3 K650E mutant (unknown origin) by radiometric kinase activity assay | | | |
| AID1880112 | Antitumor activity against mouse BaF3 cells harboring TEL-V555M-FGFR3 mutant xenografted in BALB/c mouse assessed as tumor growth inhibition at 30 mg/kg, ip qd for 15 days measured once every 2 days | | | |
| AID1880106 | Antitumor activity against mouse BaF3 cells harboring TEL-V555M-FGFR3 mutant xenografted in BALB/c mouse assessed as tumor mean volume at 30 mg/kg, po qd for 15 days measured once every 2 days (Rvb = 100%) | | | |
| AID1880116 | Stability in dog liver microsomes assessed as parent compound remaining at 1 uM incubated for 30 mins | | | |
| AID1416442 | Inhibition of wild type non-phosphorylated N-terminal His6-tagged FGFR4 (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1849312 | Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition a | | | |
| AID1458770 | Inhibition of SMO V404M mutant in gefitinib resistant human HCC827 cells assessed as decrease in GLI1 activity at 60 uM by GLI1 luciferase reporter assay relative to control | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. |
| AID1717930 | Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880021 | Inhibition of wild-type FGFR1 (unknown origin) by radiometric kinase activity assay | | | |
| AID1717901 | Drug metabolism in rat liver microsome assessed as reduction of aldehyde group at 10 mM measured after 15 mins in presence of NADPH by LC-MS analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880109 | Antitumor activity against mouse BaF3 cells harboring TEL-V555M-FGFR3 mutant xenografted in BALB/c mouse assessed as tumor mean volume at 30 mg/kg, ip qd for 15 days measured once every 2 days (Rvb = 100%) | | | |
| AID1617966 | Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell growth at 10 uM incubated for 48 hrs by MTT assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1849315 | Inhibition of recombinant human FGFR3 V555M mutant using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | | | |
| AID1431260 | Inhibition of recombinant FGFR4 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1717911 | Inhibition of FGFR4 in mouse BAF3 cells assessed as decrease in FGFR4 phosphorylation incubated for 40 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1446224 | Anticancer activity in cholangiocarcinoma patient harboring FGFR2 translocation assessed as objective response rate | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. |
| AID1717899 | Inhibition of FGFR4 in human RH41 cells assessed as decrease in phosphorylation of MAPK/ERK at 50 nM incubated for 40 mins by Western blot analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1717897 | Inhibition of FGFR4 in human RH41 cells assessed as decrease in phosphorylation of MAPK/ERK at 50 nM incubated for 3 days by Western blot analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1617962 | Inhibition of N-terminal GST-tagged human FGFR1 cytoplasmic domain (398-822 AA) expressed in baculovirus using FAM-labelled peptide as substrate pre-incubated for 10 mins followed by substrate addition by mobility shift assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1880037 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| AID1778526 | Inhibition of FGFR3 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1717900 | Inhibition of FGFR4 in human RH41 cells assessed as decrease in FRS2 phosphorylation at 50 nM incubated for 40 mins by Western blot analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880023 | Inhibition of wild-type FGFR3 (unknown origin) by radiometric kinase activity assay | | | |
| AID1416440 | Inhibition of phosphorylated FGFR2 (406 to 821 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1880038 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| AID1584403 | Antiproliferative activity against FGFR3 amplified human RT112 cells after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1880101 | Antitumor activity against human AN3-CA cells xenografted in BALB/c mouse assessed as tumor mean volume at 10 mg/kg, po qd for 15 days measured once every 2 days (Rvb = 100%) | | | |
| AID1880040 | Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| AID1431258 | Inhibition of recombinant FGFR2 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1717908 | Hepatic extraction ratio in rat liver microsomes preincubated for 3 mins followed by NADPH addition and measured after 60 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880118 | Inhibition of CYP2C9 (unknown origin) assessed as remaining activity at 10 uM relative to control | | | |
| AID1880121 | Inhibition of CYP3A4 (unknown origin) assessed as remaining activity at 10 uM relative to control | | | |
| AID1617986 | Inhibition of FGF-induced FGFR1 phosphorylation in serum-starved human H520 cells at 10 uM incubated for 1 hr by Western blot analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1416443 | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C552A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1880119 | Inhibition of CYP2C19 (unknown origin) assessed as remaining activity at 10 uM relative to control | | | |
| AID1849314 | Inhibition of recombinant human FGFR1 using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | | | |
| AID1584406 | Antiproliferative activity against mouse BAF3 cells expressing TEL-fused KDR kinase after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1584405 | Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FGFR4 kinase after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1717996 | Antiproliferative activity against human JHH7 cells assessed as reduction in cell viability by cell proliferation assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1717952 | Inhibition of FGFR4 in human Hep3B cells assessed as decrease in FRS2 phosphorylation at 500 nM incubated upto 72 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1458769 | Inhibition of SMO V404M mutant in gefitinib resistant human HCC827 cells assessed as decrease in GLI1 activity at 2 uM by GLI1 luciferase reporter assay relative to control | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. |
| AID1717951 | Inhibition of FGFR4 in human Hep3B cells assessed as decrease in phosphorylation of MAPK/ERK at 500 nM incubated up to 72 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1458771 | Inhibition of SMO V404M mutant in gefitinib resistant human HCC827 cells assessed as decrease in GLI1 activity at 2 to 60 uM in presence of SMO agonist SAG by GLI1 luciferase reporter assay | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. |
| AID1880025 | Inhibition of FGFR1 V561M mutant (unknown origin) by radiometric kinase activity assay | | | |
| AID1446225 | Anticancer activity in metastatic urothelial cancer patient harboring FGFR3 mutant or translocation assessed as objective response rate | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. |
| AID1880115 | Stability in rat liver microsomes assessed as parent compound remaining at 1 uM incubated for 30 mins | | | |
| AID1617965 | Antiproliferative activity against human NCI-H520 cells assessed as inhibition of cell growth at 10 uM incubated for 48 hrs by MTT assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1849335 | Inhibition of recombinant human FGFR4 (460 to 802 residues) using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | | | |
| AID1446214 | In vivo inhibition of FGFR2 in rat assessed as reduction in bFGF-induced CCL2 production at 10 mg/kg, po measured at 12 hrs post dose relative to control | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. |
| AID1431257 | Inhibition of recombinant FGFR1 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1717910 | Inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability incubated for 2 days by cell proliferation assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880113 | Stability in human liver microsomes assessed as parent compound remaining at 1 uM incubated for 30 mins | | | |
| AID1458765 | Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. |
| AID1880114 | Stability in mouse liver microsomes assessed as parent compound remaining at 1 uM incubated for 30 mins | | | |
| AID1617987 | Inhibition of FGFR in serum-starved human H520 cells assessed as reduction in FGFR-induced AKT phosphorylation at 10 uM incubated for 1 hr by Western blot analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1416444 | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C477A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1717902 | Drug metabolism in human liver microsome assessed as reduction of aldehyde group at 10 mM measured after 15 mins in presence of NADPH by LC-MS analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880117 | Inhibition of CYP1A2 (unknown origin) assessed as remaining activity at 10 uM relative to control | | | |
| AID1416441 | Inhibition of phosphorylated FGFR3 (411 to 806 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1880039 | Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| AID1718007 | Selectivity ratio of IC50 for antiproliferative activity against human HUH7 cells to IC50 for inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1717898 | Inhibition of FGFR4 in human RH41 cells assessed as decrease in FRS2 phosphorylation at 50 nM incubated for 3 days by Western blot analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1717909 | Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by cell proliferation assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880027 | Inhibition of FGFR3 V555M mutant (unknown origin) by radiometric kinase activity assay | | | |
| AID1446125 | In vivo inhibition of FGFR2 in rat assessed as reduction in bFGF-induced CCL2 production at 10 mg/kg, po measured at 5 hrs post dose relative to control | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. |
| AID1717896 | Permeability of the compound in human Caco-2 cells assessed as compound recovery at 10 uM measured after 2 hrs by LC/MS/MS analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1849313 | Inhibition of recombinant human FGFR3 V555L mutant using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay | | | |
| AID1617964 | Antiproliferative activity against human PC9 cells assessed as inhibition of cell growth at 10 uM incubated for 48 hrs by MTT assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1617967 | Antiproliferative activity against human NCI-H226 cells assessed as inhibition of cell growth at 10 uM incubated for 48 hrs by MTT assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1880031 | Inhibition of FGFR2 V564F mutant (unknown origin) at 10 uM by radiometric kinase activity assay relative to control | | | |
| AID1458764 | Displacement of [3H]-cyclopamine from human wild-type SMO receptor expressed in HEK293T cell membranes by liquid scintillation spectrometry | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. |
| AID1778524 | Inhibition of FGFR1 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1880024 | Inhibition of wild-type FGFR4 (unknown origin) by radiometric kinase activity assay | | | |
| AID1880035 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| 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. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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. |
| 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. |
| 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. |
| AID1345506 | Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
| AID1345535 | Human fibroblast growth factor receptor 3 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
| AID1345514 | Human fibroblast growth factor receptor 1 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
| AID1345568 | Human fibroblast growth factor receptor 4 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
| AID1345517 | Human fibroblast growth factor receptor 2 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |