tasurgratinib [Ligand Id: 11414] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3686884 (E 7090, E-7090, E7090, Tasurgratinib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Fibroblast growth factor 2 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) |
| ChEMBL | Cell-Free Kinase Inhibitory Activity: To a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 μl of FGFR1 protein (Carna Biosciences, Inc., 08-133) solution diluted to 1 μg/mL with an assay buffer (20 mM HEPES-NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 μL 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 μM, and 5 μl of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour. For measuring kinase activity, ADP-Glo¿ Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 μL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at room temperature for 40 minutes to stop the kinase reaction and to deplete the remaining ATP. The kinase detection reagent was further added, and the reaction was performed at room temperature for 40 minutes, so as to cause conversion from ADP to ATP, a luciferase/luciferin coupling reaction and a luminous reaction by ATP. To evaluate the enzyme activity, the amount of luminescence in each well was measured by Envision¿ (PerkinElmer Co., Ltd.). The luminescence values of the wells containing the kinase protein without adding the test substance was defined as 100% and the luminescence values of the wells adding neither the test substance nor the kinase protein was defined as 0%. Then, a luminescence value ratio in the presence of the test substance was calculated. On the basis of this luminescence value ratio, the concentration of the test substance necessary for inhibiting the kinase activity by 50% (i.e., an IC50 value) was calculated.FGFR2 cell-free kinase inhibitory activity, FGFR3 cell-free kinase inhibitory activity, and FGFR4 cell-free kinase inhibitory activity were measured respectively by using FGFR2 protein (Carna Biosciences, Inc., 08-134), FGFR3 protein (Carna Biosciences, Inc., 08-135), or FGFR4 protein (Carna Biosciences, Inc., 08-136) in the same manner as the case of the aforementioned FGFR1 cell-free kinase inhibitory activity. However, with respect to a concentration of ATP, cell-free kinase inhibitory activity were evaluated in a final concentration of 35 μM for FGFR2, in a final concentration of 16.7 μM for FGFR3, and in a final concentration of 75 μM for FGFR4. For FGFR3 and FGFR4, the reaction with the test substance was performed at room temperature for 2 hours. | B | 8.24 | pIC50 | 5.7 | nM | IC50 | US-9951047-B2. Salt of monocyclic pyridine derivative and crystal thereof (2018) |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Cell-Free Kinase Inhibitory Activity: To a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 μl of FGFR1 protein (Carna Biosciences, Inc., 08-133) solution diluted to 1 μg/mL with an assay buffer (20 mM HEPES-NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 μL 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 μM, and 5 μl of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour. For measuring kinase activity, ADP-Glo¿ Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 μL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at room temperature for 40 minutes to stop the kinase reaction and to deplete the remaining ATP. The kinase detection reagent was further added, and the reaction was performed at room temperature for 40 minutes, so as to cause conversion from ADP to ATP, a luciferase/luciferin coupling reaction and a luminous reaction by ATP. To evaluate the enzyme activity, the amount of luminescence in each well was measured by Envision¿ (PerkinElmer Co., Ltd.). The luminescence values of the wells containing the kinase protein without adding the test substance was defined as 100% and the luminescence values of the wells adding neither the test substance nor the kinase protein was defined as 0%. Then, a luminescence value ratio in the presence of the test substance was calculated. On the basis of this luminescence value ratio, the concentration of the test substance necessary for inhibiting the kinase activity by 50% (i.e., an IC50 value) was calculated.FGFR2 cell-free kinase inhibitory activity, FGFR3 cell-free kinase inhibitory activity, and FGFR4 cell-free kinase inhibitory activity were measured respectively by using FGFR2 protein (Carna Biosciences, Inc., 08-134), FGFR3 protein (Carna Biosciences, Inc., 08-135), or FGFR4 protein (Carna Biosciences, Inc., 08-136) in the same manner as the case of the aforementioned FGFR1 cell-free kinase inhibitory activity. However, with respect to a concentration of ATP, cell-free kinase inhibitory activity were evaluated in a final concentration of 35 μM for FGFR2, in a final concentration of 16.7 μM for FGFR3, and in a final concentration of 75 μM for FGFR4. For FGFR3 and FGFR4, the reaction with the test substance was performed at room temperature for 2 hours. | B | 8.29 | pIC50 | 5.1 | nM | IC50 | US-9951047-B2. Salt of monocyclic pyridine derivative and crystal thereof (2018) |
| GtoPdb | - | - | 8.35 | pIC50 | 4.5 | 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 | Cell-Free Kinase Inhibitory Activity: To a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 μl of FGFR1 protein (Carna Biosciences, Inc., 08-133) solution diluted to 1 μg/mL with an assay buffer (20 mM HEPES-NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 μL 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 μM, and 5 μl of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour. For measuring kinase activity, ADP-Glo¿ Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 μL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at room temperature for 40 minutes to stop the kinase reaction and to deplete the remaining ATP. The kinase detection reagent was further added, and the reaction was performed at room temperature for 40 minutes, so as to cause conversion from ADP to ATP, a luciferase/luciferin coupling reaction and a luminous reaction by ATP. To evaluate the enzyme activity, the amount of luminescence in each well was measured by Envision¿ (PerkinElmer Co., Ltd.). The luminescence values of the wells containing the kinase protein without adding the test substance was defined as 100% and the luminescence values of the wells adding neither the test substance nor the kinase protein was defined as 0%. Then, a luminescence value ratio in the presence of the test substance was calculated. On the basis of this luminescence value ratio, the concentration of the test substance necessary for inhibiting the kinase activity by 50% (i.e., an IC50 value) was calculated.FGFR2 cell-free kinase inhibitory activity, FGFR3 cell-free kinase inhibitory activity, and FGFR4 cell-free kinase inhibitory activity were measured respectively by using FGFR2 protein (Carna Biosciences, Inc., 08-134), FGFR3 protein (Carna Biosciences, Inc., 08-135), or FGFR4 protein (Carna Biosciences, Inc., 08-136) in the same manner as the case of the aforementioned FGFR1 cell-free kinase inhibitory activity. However, with respect to a concentration of ATP, cell-free kinase inhibitory activity were evaluated in a final concentration of 35 μM for FGFR2, in a final concentration of 16.7 μM for FGFR3, and in a final concentration of 75 μM for FGFR4. For FGFR3 and FGFR4, the reaction with the test substance was performed at room temperature for 2 hours. | B | 8.22 | pIC50 | 6 | nM | IC50 | US-9951047-B2. Salt of monocyclic pyridine derivative and crystal thereof (2018) |
| 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] | ||||||||
| ChEMBL | Cell-Free Kinase Inhibitory Activity: To a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 μl of FGFR1 protein (Carna Biosciences, Inc., 08-133) solution diluted to 1 μg/mL with an assay buffer (20 mM HEPES-NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 μL 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 μM, and 5 μl of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour. For measuring kinase activity, ADP-Glo¿ Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 μL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at room temperature for 40 minutes to stop the kinase reaction and to deplete the remaining ATP. The kinase detection reagent was further added, and the reaction was performed at room temperature for 40 minutes, so as to cause conversion from ADP to ATP, a luciferase/luciferin coupling reaction and a luminous reaction by ATP. To evaluate the enzyme activity, the amount of luminescence in each well was measured by Envision¿ (PerkinElmer Co., Ltd.). The luminescence values of the wells containing the kinase protein without adding the test substance was defined as 100% and the luminescence values of the wells adding neither the test substance nor the kinase protein was defined as 0%. Then, a luminescence value ratio in the presence of the test substance was calculated. On the basis of this luminescence value ratio, the concentration of the test substance necessary for inhibiting the kinase activity by 50% (i.e., an IC50 value) was calculated.FGFR2 cell-free kinase inhibitory activity, FGFR3 cell-free kinase inhibitory activity, and FGFR4 cell-free kinase inhibitory activity were measured respectively by using FGFR2 protein (Carna Biosciences, Inc., 08-134), FGFR3 protein (Carna Biosciences, Inc., 08-135), or FGFR4 protein (Carna Biosciences, Inc., 08-136) in the same manner as the case of the aforementioned FGFR1 cell-free kinase inhibitory activity. However, with respect to a concentration of ATP, cell-free kinase inhibitory activity were evaluated in a final concentration of 35 μM for FGFR2, in a final concentration of 16.7 μM for FGFR3, and in a final concentration of 75 μM for FGFR4. For FGFR3 and FGFR4, the reaction with the test substance was performed at room temperature for 2 hours. | B | 6.17 | pIC50 | 683 | nM | IC50 | US-9951047-B2. Salt of monocyclic pyridine derivative and crystal thereof (2018) |
| 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) |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
