tasurgratinib [Ligand Id: 11414] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3686884 (E7090, E-7090)
  • Basic fibroblast growth factor in Human [ChEMBL: CHEMBL3107] [UniProtKB: P09038]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
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  • fibroblast growth factor receptor 2 in Human [GtoPdb: 1809] [UniProtKB: P21802]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Basic fibroblast growth factor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3107] [UniProtKB: P09038]
ChEMBL ADP-Glo Kinase Assay: In this assay, the inhibitory activity of a test substance against the tyrosine kinase activity of FGFR2 protein is measured.To each well of a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 ul of FGFR2 protein (Cama Biosciences, Inc., 08434) solution diluted to 1 ug/mL with an assay buffer (20 mM HEPES-NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 uL of an assay buffer solution containing CSK-tide substrate (Ana Spec Inc., 63843) in a final concentration of 1000 nM and ATP (Promega Corporation, V9102) in a final concentration of 35 uM, and 5 ul of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour (kinase reaction). For measuring kinase activity, ADP-Glo Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 uL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at room temperature for 40 minutes. B 8.35 pIC50 4.5 nM IC50 US-8933099-B2. Monocyclic pyridine derivative (2015)
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL ADP-Glo Kinase Assay: In this assay, the inhibitory activity of a test substance against the tyrosine kinase activity of FGFR1 protein is measured.To each well of a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 ul of FGFR1 protein (Cama Biosciences, Inc., 08-133) solution diluted to 1 ug/mL with an assay buffer (20 mM HEPES NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 ul, of an assay buffer solution containing CSK-tide substrate (Ana Spec Inc., 63843) in a final concentration of 1000 nM and ATP (Promega Corporation, V9102) in a final concentration of 58.3 uM, and 5 ul of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour (kinase reaction). For measuring kinase activity, ADP-Glo Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 uL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at morn temperature for 40 minutes. B 8.24 pIC50 5.8 nM IC50 US-8933099-B2. Monocyclic pyridine derivative (2015)
GtoPdb - - 8.24 pIC50 5.8 nM IC50 WO2014129477A1. Monocyclic pyridine derivative (2014)
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
ChEMBL ADP-Glo Kinase Assay: In this assay, the inhibitory activity of a test substance against the tyrosine kinase activity of FGFR3 protein is measured.To each well of a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 ul of FGFR3 protein (Cama Biosciences, Inc., 08-135) solution diluted to 1 ug/mL with an assay buffer (20 mM HEPES NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 uL of an assay buffer solution containing CSK-tide substrate (Ana Spec Inc., 63843) in a final concentration 011000 nM and ATP (Promega Corporation, V9102) in a final concentration of 16.7 uM, and 5 ul of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 2 hours (kinase reaction). For measuring kinase activity, ADP-Glo Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 pt of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at room temperature for 40 minutes. B 8.27 pIC50 5.4 nM IC50 US-8933099-B2. Monocyclic pyridine derivative (2015)
GtoPdb - - 8.27 pIC50 5.4 nM IC50 WO2014129477A1. Monocyclic pyridine derivative (2014)
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
GtoPdb - - 6.19 pIC50 644 nM IC50 WO2014129477A1. Monocyclic pyridine derivative (2014)
ChEMBL ADP-Glo Kinase Assay: In this assay, the inhibitory activity of a test substance against the tyrosine kinase activity of FGFR4 protein is measured.To each well of a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 ul FGFR4 protein (Carna Biosciences, Inc., 08-136) solution diluted to 1 ug/mL with an assay buffer (20 mM HEPES-NaOH, 0.01% Triton X-100, 2 mM DTT, 5 mM MgCl2 and 2 mM MnCl2), 10 uL of an assay buffer solution containing CSK-tide substrate (Ana Spec Inc., 63843) in a final concentration of 1000 nM and ATP (Promega Corporation, V9102) in a final concentration of 75 uM, and 5 ul of a test substance diluted with the assay buffer were added and the reaction was performed at room temperature for 2 hours (kinase reaction). For measuring kinase activity, ADP-Glo Kinase Assay (Promega Corporation, V9102) was used. B 6.19 pIC50 644.5 nM IC50 US-8933099-B2. Monocyclic pyridine derivative (2015)
fibroblast growth factor receptor 2 in Human [GtoPdb: 1809] [UniProtKB: P21802]
GtoPdb - - 8.35 pIC50 4.5 nM IC50 WO2014129477A1. Monocyclic pyridine derivative (2014)

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]