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ChEMBL ligand: CHEMBL3701238 (Fgfr-in-1, Futibatinib, Lytgobi, Tas 120, Tas-120, TAS-120) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of recombinant human EGFR del19/T790M using biotinEEPLYWSFPAKKK-NH2 as substrate incubated for 120 mins by TR-FRET assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | ACS Med Chem Lett (2023) 14: 396-404 [PMID:37077386] |
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
ChEMBL | Inhibition of FGFR1 (unknown origin) | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (2022) 65: 58-83 [PMID:34962782] |
ChEMBL | Inhibition of human recombinant FGFR1 expressed in Escherichia coli BL21 DE3 assessed as inhibition by western blot analysis | B | 8.41 | pIC50 | 3.9 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
GtoPdb | - | - | 8.44 | pIC50 | 3.6 | nM | IC50 | WO2013108809. 3,5-disubstituted alkynylbenzene compound and salt thereof (2013) |
ChEMBL | Inhibition Assay: Purified recombinant human FGFR4 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR4 kinase activity, a biotinylated peptide (biotin-EEPLYWSFPAKKK) was synthesized for use as a substrate by utilizing the amino acid sequence of FL-Peptide 22 (Caliper Life Sciences, Inc.) with biotin. The purified recombinant human FGFR4 protein used in the test was purchased from Carna Biosciences, Inc. In the measurement of the inhibitory effect of the compounds, first, a test compound was gradually diluted with dimethylsulfoxide (DMSO) to a concentration 20 times higher than the final concentration. Next, the purified human FGFR4 protein, substrate peptide (final concentration: 250 nM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 190 .mu.M), and the test compound DMSO solution (final concentration of DMSO: 5%) were added to a reaction buffer. | B | 8.44 | pIC50 | 3.6 | nM | IC50 | US-9108973-B2. 3,5-disubstituted alkynylbenzene compound and salt thereof (2015) |
ChEMBL | Inhibition of human FGFR1 (459 to 765 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2021) 64: 9078-9099 [PMID:34129329] |
ChEMBL | Inhibition of human FGFR1 | B | 8.74 | pIC50 | 1.8 | nM | IC50 | ACS Med Chem Lett (2023) 14: 396-404 [PMID:37077386] |
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
ChEMBL | Inhibition of human FGFR2 (458 to 768 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | B | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2021) 64: 9078-9099 [PMID:34129329] |
ChEMBL | Inhibition of recombinant wild type FGFR2 (unknown origin) | B | 8.4 | pIC50 | <4 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
ChEMBL | Inhibition of human recombinant cytoplasmic domain FGFR2 (8 to 134 residues) incubated for 120 mins by mobility shift assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | ACS Med Chem Lett (2023) 14: 396-404 [PMID:37077386] |
ChEMBL | Inhibition of human recombinant FGFR2 expressed in Escherichia coli BL21 DE3 assessed as inhibition by western blot analysis | B | 8.89 | pIC50 | 1.3 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
ChEMBL | Inhibition of FGFR2 (unknown origin) | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2022) 65: 58-83 [PMID:34962782] |
ChEMBL | Inhibition Assay: When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences, Inc.) was used as a substrate. The purified recombinant human FGFR2 protein used in the test was purchased from Carna Biosciences, Inc. In the measurement of the inhibitory effect of the compounds, first, a test compound was gradually diluted with dimethylsulfoxide (DMSO) to a concentration that was 20 times higher than the final concentration. Next, the purified human FGFR2 protein, FL-Peptide 22 (final concentration: 1.5 .mu.M), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 .mu.M), and the test compound DMSO solution (final concentration of DMSO: 5%) were added to a reaction buffer (15 mM Tris-HCl pH 7.5, 0.01% Tween-20, 2 mM DTT), and the mixture was incubated at 25.degree. C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer. | B | 8.96 | pIC50 | 1.1 | nM | IC50 | US-9108973-B2. 3,5-disubstituted alkynylbenzene compound and salt thereof (2015) |
GtoPdb | - | - | 8.96 | pIC50 | 1.1 | nM | IC50 | WO2013108809. 3,5-disubstituted alkynylbenzene compound and salt thereof (2013) |
ChEMBL | Inhibition of human recombinant cytoplasmic domain FGFR2 (8 to 134 residues) incubated for 120 mins by mobility shift assay | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2023) 14: 396-404 [PMID:37077386] |
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
ChEMBL | Inhibition of FGFR3 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2022) 65: 58-83 [PMID:34962782] |
ChEMBL | Inhibition of human recombinant FGFR3 expressed in Escherichia coli BL21 DE3 assessed as inhibition by western blot analysis | B | 8.8 | pIC50 | 1.6 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
ChEMBL | Inhibition of human FGFR3 | B | 8.8 | pIC50 | 1.6 | nM | IC50 | ACS Med Chem Lett (2023) 14: 396-404 [PMID:37077386] |
ChEMBL | Inhibition of human FGFR3 (450 to 758 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | B | 9.28 | pIC50 | 0.53 | nM | IC50 | J Med Chem (2021) 64: 9078-9099 [PMID:34129329] |
GtoPdb | - | - | 9.3 | pIC50 | 0.5 | nM | IC50 | WO2013108809. 3,5-disubstituted alkynylbenzene compound and salt thereof (2013) |
ChEMBL | Inhibition Assay: Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR3 kinase activity, a biotinylated peptide (biotin-EEPLYWSFPAKKK) was synthesized for use as a substrate by utilizing the amino acid sequence of FL-Peptide 22 (Caliper Life Sciences, Inc.) with biotin. The purified recombinant human FGFR3 protein used in the test was purchased from Carna Biosciences, Inc. In the measurement of the inhibitory effect of the compounds, first, a test compound was gradually diluted with dimethylsulfoxide (DMSO) to a concentration 20 times higher than the final concentration. Next, the purified human FGFR3 protein, substrate peptide (final concentration: 250 nM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 190 .mu.M), and the test compound DMSO solution (final concentration of DMSO: 5%) were added to a reaction buffer. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9108973-B2. 3,5-disubstituted alkynylbenzene compound and salt thereof (2015) |
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
ChEMBL | Inhibition of FGFR4 (unknown origin) | B | 8.08 | pIC50 | 8.3 | nM | IC50 | J Med Chem (2022) 65: 58-83 [PMID:34962782] |
ChEMBL | Inhibition of human recombinant FGFR4 expressed in Escherichia coli BL21 DE3 assessed as inhibition by western blot analysis | B | 8.08 | pIC50 | 8.3 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
ChEMBL | Inhibition of human FGFR4 (445 to 753 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (2021) 64: 9078-9099 [PMID:34129329] |
ChEMBL | Inhibition of human FGFR4 | B | 8.43 | pIC50 | 3.7 | nM | IC50 | ACS Med Chem Lett (2023) 14: 396-404 [PMID:37077386] |
ChEMBL | Inhibition Assay: Purified recombinant human FGFR4 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR4 kinase activity, a biotinylated peptide (biotin-EEPLYWSFPAKKK) was synthesized for use as a substrate by utilizing the amino acid sequence of FL-Peptide 22 (Caliper Life Sciences, Inc.) with biotin. The purified recombinant human FGFR4 protein used in the test was purchased from Carna Biosciences, Inc. In the measurement of the inhibitory effect of the compounds, first, a test compound was gradually diluted with dimethylsulfoxide (DMSO) to a concentration 20 times higher than the final concentration. Next, the purified human FGFR4 protein, substrate peptide (final concentration: 250 nM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 190 .mu.M), and the test compound DMSO solution (final concentration of DMSO: 5%) were added to a reaction buffer. | B | 8.47 | pIC50 | 3.4 | nM | IC50 | US-9108973-B2. 3,5-disubstituted alkynylbenzene compound and salt thereof (2015) |
GtoPdb | - | - | 8.47 | pIC50 | 3.4 | nM | IC50 | WO2013108809. 3,5-disubstituted alkynylbenzene compound and salt thereof (2013) |
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
ChEMBL | Inhibition of BTK (unknown origin) measured by ADP-Glo assay | B | 7.02 | pIC50 | 94.9 | nM | IC50 | Eur J Med Chem (2022) 241: 114611-114611 [PMID:35939993] |
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
ChEMBL | Inhibition of N-terminal GST tagged recombinant human VEGFR2 (aa805 to 1356 residues) expressed in baculovirus expression system using Poly- (Glu4:Tyr)-biotin as substrate incubated for 80 mins in presence of ATP by kinase glo method | B | 5.63 | pIC50 | 2358 | nM | IC50 | ACS Med Chem Lett (2023) 14: 396-404 [PMID:37077386] |
ChEMBL data shown on this page come from version 34:
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]