| Assay ID | Title | Year | Journal | Article |
|---|
| AID1516681 | Antiproliferative activity against human UMUC14 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1193347 | Cytotoxicity against human HL7702 cells assessed as cell survival at 2 to 10 uM after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1313608 | Inhibition of recombinant human VEGFR2 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1626475 | Inhibition of human FGFR2 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1626488 | Antitumor activity against human NCI-H1581 cells xenografted in nude mouse assessed as tumor growth inhibition at 12.5 mg/kg, po qd administered for 21 days | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| 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. |
| 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. |
| AID1176848 | Inhibition of FGFR2 (unknown origin) at 10 nM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID1316518 | Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of novel arylaminoquinazolinylurea derivatives and their antiproliferative activities against bladder cancer cell line. |
| AID1584401 | Antiproliferative activity against FGFR2 amplified human SNU16 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. |
| 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. |
| AID1193339 | Inhibition of FGFR1 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1298508 | Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1626474 | Volume of distribution in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1484911 | Inhibition of FGFR1 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
| AID1431267 | Inhibition of recombinant human FGFR4 in presence of ATP | 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. |
| AID1426086 | Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer. |
| AID1193340 | Inhibition of FGFR2 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| 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. |
| AID1613015 | Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1845304 | Inhibition of recombinant human FGFR4 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1313644 | Antitumor activity against human NCI-H1581 cells xenografted in nude mouse assessed as tumor growth inhibition at 20 mg/kg administered as qd for 21 days measured on day 21 post last dose relative to vehicle-treated control | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1313641 | Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1404606 | Antiproliferative activity against human SNU16 cells expressing FGFR2 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1298518 | Inhibition of recombinant FGFR4 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1313606 | Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1717976 | Inhibition of wild-type FGFR4 (unknown origin) assessed as ratio of Kinact to Ki | 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. |
| AID1626497 | Inhibition of human FGFR2 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1626470 | Cmax in ICR mouse at 12.5 mg/kg administered as oral gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1431265 | Inhibition of recombinant human FGFR2 in presence of ATP | 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. |
| AID1450773 | Inhibition of FGFR2 in human SNU16 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626491 | Protein binding in mouse plasma at 5 uM after 4 hrs by equilibrium dialysis assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1516684 | Antiproliferative activity against mouse BaF3/TEL-VEGFR2 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1313605 | Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1404604 | Antiproliferative activity against human KG1 cells expressing FGFR1 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1810715 | Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1431266 | Inhibition of recombinant human FGFR3 in presence of ATP | 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. |
| AID1613014 | Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1404607 | Antiproliferative activity against human RT112 cells expressing FGFR3 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1810713 | Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1845305 | Inhibition of recombinant human KDR in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1298506 | Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| 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. |
| AID1298524 | Inhibition of FGFR1 in human KG1 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| 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. |
| AID1298523 | Inhibition of FGFR1 in human H1581 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1626468 | AUC(0 to infinity) in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1487617 | Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1404609 | Antiproliferative activity against mouse BAF3 cells expressing VEGFR2 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1845302 | Inhibition of recombinant human FGFR2 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1516666 | Inhibition of human VEGFR2 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1584423 | Inhibition of FGFR4 (unknown origin) | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) 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. |
| AID1516661 | Inhibition of human FGFR1 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1450763 | Inhibition of FGFR1OP2 fused FGFR1 in human KG1 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1810704 | Inhibition of human FGFR3 (450 to 758 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1613038 | Inhibition of FGFR2 phosphorylation in human SNU-16 cells at 50 nM after 2 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1584402 | Antiproliferative activity against FGFR3 amplified human OPM2 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. |
| AID1626462 | Inhibition of recombinant human FGFR1 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase 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. |
| AID1626500 | Inhibition of human VEGFR2 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1516665 | Inhibition of human FGFR4 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1487616 | Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1717977 | Inhibition of wild-type FGFR4 C477A mutant (unknown origin) assessed as ratio of Kinact to Ki | 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. |
| AID1584379 | Antiproliferative activity against FGFR1 amplified human NCI-H1581 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. |
| AID1450766 | Inhibition of FGFR3 in human RT112 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1810714 | Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1626487 | Antiproliferative activity against human RT112 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1404608 | Antiproliferative activity against human UM-UC-14 cells expressing FGFR3 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1450764 | Inhibition of FGFR2 in human KATO III cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626484 | Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1435470 | Antitumor activity against FGFR1-amplified human NCI-H1581 cells xenografted in nude mouse assessed as tumor growth inhibition at 20 mg/kg, po qd administered for 10 days and measured on day 10 post last dose relative to vehicle-treated control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
| AID1626467 | Half life in ICR mouse at 12.5 mg/kg administered as oral gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1516663 | Inhibition of human FGFR2 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1626476 | Inhibition of human FGFR3 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1810702 | Inhibition of human FGFR1 (459 to 765 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1193342 | Inhibition of FGFR4 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1516683 | Antiproliferative activity against mouse BaF3/TEL-FGFR1 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1193343 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1626471 | AUC(0 to infinity) in ICR mouse at 12.5 mg/kg administered as oral gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1313640 | Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1487618 | Inhibition of recombinant FGFR2 (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA based spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1313639 | Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1450705 | Inhibition of recombinant human FGFR3 using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626464 | Antiproliferative activity against human NCI-H1581 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1404603 | Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA based spectrophotometric method | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1450703 | Inhibition of recombinant human FGFR1 using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626472 | Clearance in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1613017 | Antiproliferative activity against human UM-UC-14 cells harboring FGFR3 mutation after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1450735 | Inhibition of FGFR1 in human NCI-H1581 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1404605 | Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1626498 | Inhibition of human FGFR3 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1845303 | Inhibition of recombinant human FGFR3 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1626485 | Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1298525 | Inhibition of FGFR2 in human KATO III cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1516662 | Antiproliferative activity against human KG1 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1584377 | Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1313647 | Inhibition of recombinant human FGFR4 | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1626477 | Inhibition of human FGFR4 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1298517 | Inhibition of recombinant FGFR3 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1450704 | Inhibition of recombinant human FGFR2 using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1176847 | Inhibition of FGFR1 (unknown origin) at 10 nM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID1298515 | Selectivity ratio of IC50 for recombinant VEGFR2 (unknown origin) to IC50 for recombinant FGFR2 (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1810716 | Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1516695 | Irreversible inhibition of human FGFR1 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by caliper assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| 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. |
| AID1845301 | Inhibition of recombinant human FGFR1 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1626466 | Half life in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1810717 | Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1426088 | Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer. |
| AID1298516 | Inhibition of recombinant FGFR1 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| 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. |
| AID1778528 | Inhibition of recombinant human FGFR1 in presence of ATP at Km concentration | 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. |
| AID1626463 | Inhibition of recombinant human VEGFR2 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| 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. |
| AID1810705 | Inhibition of human FGFR4 (445 to 753 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1845250 | Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1626473 | Oral bioavailability in ICR mouse at 12.5 mg/kg administered as gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1313609 | Selectivity ratio of IC50 for recombinant human VEGFR2 to IC50 for recombinant human FGFR1 | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1516664 | Inhibition of human FGFR3 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1778530 | Inhibition of recombinant human FGFR3 in presence of ATP at Km concentration | 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. |
| 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. |
| AID1193341 | Inhibition of FGFR3 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1487619 | Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA based spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1516682 | Antiproliferative activity against human SNU16 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1193344 | Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1626496 | Inhibition of human FGFR1 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1298526 | Inhibition of FGFR3 in human RT112 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor 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. |
| AID1193345 | Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1626486 | Antiproliferative activity against human KATO III cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| 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. |
| AID1426087 | Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer. |
| AID1193346 | Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1431264 | Inhibition of recombinant human FGFR1 in presence of ATP | 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. |
| AID1612907 | Inhibition of FGFR1 (unknown origin) after 60 mins by ELISA | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1298514 | Inhibition of recombinant VEGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
| Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1613016 | Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1810703 | Inhibition of human FGFR2 (458 to 768 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Discovery and Optimization of a Novel 2 |
| AID1626499 | Inhibition of human FGFR4 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase 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. |
| AID1778529 | Inhibition of recombinant human FGFR2 in presence of ATP at Km concentration | 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. |
| AID1626469 | Cmax in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1450765 | Inhibition of FGFR3 mutant in human UM-UC-14 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| 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. |
| 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. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1345514 | Human fibroblast growth factor receptor 1 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2015 | Organic & biomolecular chemistry, Jul-28, Volume: 13, Issue:28
| Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |