ChEMBL ligand: CHEMBL3701238 (Fgfr-in-1, Futibatinib, Lytgobi, Tas 120, Tas-120, TAS-120)
epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] There should be some charts here, you may need to enable JavaScript!
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
epidermal growth factor receptor/Epidermal growth factor receptor 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 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]
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 FGFR1 (unknown origin)	B	8.41	pIC50	3.9	nM	IC50	Eur J Med Chem (2024) 275: 116612-116612 [PMID:38908103]
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	Measurement of Inhibitory Effect on FGFR1 Kinase Activity: When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR1 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 FGFR1 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 FGFR1 protein, substrate peptide (final concentration: 250 nM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 190 μM), 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° C. for 120 minutes to perform a kinase reaction. EDTA was added thereto to a final concentration of 40 mM to thereby terminate the reaction. Then, a detection solution containing Eu-labeled anti-phosphorylated tyrosine antibody PT66 (PerkinElmer) and SureLight APC-SA (PerkinElmer) was added, and the resulting mixture was allowed to stand at room temperature for 2 hours or more. Finally, the intensity of fluorescence when excitation light with a wavelength of 337 nm was irradiated was measured by a PHERAstar FS (BMG LABTECH) at two wavelengths of 620 nm and 665 nm. The amount of phosphorylation was determined from the fluorescence intensity ratio of the two wavelengths. The compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM).	B	8.44	pIC50	3.6	nM	IC50	US-10894048-B2. Antitumor drug for intermittent administration of FGFR inhibitor (2021)
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	FGFR2 Kinase Activity: 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 μM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 μM), 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° C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer (Caliper Life Sciences, Inc.) was added thereto to terminate the kinase reaction. Finally, using a LabChip (registered trademark) 3000 system (Caliper Life Sciences, Inc.; excitation wavelength: 488 nm, detection wavelength: 530 nm), phosphorylated peptides and non-phosphorylated peptides were separated, and the amount of each peptide was measured. The level of phosphorylation was determined from the quantitative ratio. The compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM).	B	6.72	pIC50	190	nM	IC50	US-10124003-B2. Therapeutic agent for FGFR inhibitor-resistant cancer (2018)
ChEMBL	Measurement of Inhibitory Effect on FGFR2 Kinase Activity: 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 μM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 μM), 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° C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer (Caliper Life Sciences, Inc.) was added thereto to terminate the kinase reaction. Finally, using a LabChip (registered trademark) 3000 system (Caliper Life Sciences, Inc.; excitation wavelength: 488 nm, detection wavelength: 530 nm), phosphorylated peptides and non-phosphorylated peptides were separated, and the amount of each peptide was measured. The level of phosphorylation was determined from the quantitative ratio. The compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM).	B	8.31	pIC50	4.9	nM	IC50	US-10894048-B2. Antitumor drug for intermittent administration of FGFR inhibitor (2021)
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 FGFR2 (unknown origin)	B	8.89	pIC50	1.3	nM	IC50	J Med Chem (2022) 65: 58-83 [PMID:34962782]
ChEMBL	Inhibition of FGFR2 (unknown origin)	B	8.89	pIC50	1.3	nM	IC50	Eur J Med Chem (2024) 275: 116612-116612 [PMID:38908103]
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	FGFR2 Kinase Activity: 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 μM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 μM), 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° C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer (Caliper Life Sciences, Inc.) was added thereto to terminate the kinase reaction. Finally, using a LabChip (registered trademark) 3000 system (Caliper Life Sciences, Inc.; excitation wavelength: 488 nm, detection wavelength: 530 nm), phosphorylated peptides and non-phosphorylated peptides were separated, and the amount of each peptide was measured. The level of phosphorylation was determined from the quantitative ratio. The compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM).	B	8.96	pIC50	1.1	nM	IC50	US-10124003-B2. Therapeutic agent for FGFR inhibitor-resistant cancer (2018)
ChEMBL	Measurement of Inhibitory Effect on FGFR2 Kinase Activity: 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 μM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 μM), 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° C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer (Caliper Life Sciences, Inc.) was added thereto to terminate the kinase reaction. Finally, using a LabChip (registered trademark) 3000 system (Caliper Life Sciences, Inc.; excitation wavelength: 488 nm, detection wavelength: 530 nm), phosphorylated peptides and non-phosphorylated peptides were separated, and the amount of each peptide was measured. The level of phosphorylation was determined from the quantitative ratio. The compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM).	B	8.96	pIC50	1.1	nM	IC50	US-10835536-B2. Therapeutic agent for FGFR inhibitor-resistant cancer (2020)
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)
ChEMBL	Measurement of Inhibitory Effect on FGFR2 Kinase Activity: 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 μM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 μM), 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° C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer (Caliper Life Sciences, Inc.) was added thereto to terminate the kinase reaction. Finally, using a LabChip (registered trademark) 3000 system (Caliper Life Sciences, Inc.; excitation wavelength: 488 nm, detection wavelength: 530 nm), phosphorylated peptides and non-phosphorylated peptides were separated, and the amount of each peptide was measured. The level of phosphorylation was determined from the quantitative ratio. The compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM).	B	8.96	pIC50	1.1	nM	IC50	US-10894048-B2. Antitumor drug for intermittent administration of FGFR inhibitor (2021)
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 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 FGFR3 (unknown origin)	B	8.8	pIC50	1.6	nM	IC50	J Med Chem (2022) 65: 58-83 [PMID:34962782]
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 FGFR3 (unknown origin)	B	8.8	pIC50	1.6	nM	IC50	Eur J Med Chem (2024) 275: 116612-116612 [PMID:38908103]
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	Measurement of Inhibitory Effect on FGFR3 Kinase Activity: The inhibitory effect of the compounds on FGFR3 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. The final concentration of ATP was 50 μM.	B	9.3	pIC50	0.5	nM	IC50	US-10894048-B2. Antitumor drug for intermittent administration of FGFR inhibitor (2021)
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 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 FGFR4 (unknown origin)	B	8.08	pIC50	8.3	nM	IC50	J Med Chem (2022) 65: 58-83 [PMID:34962782]
ChEMBL	Inhibition of FGFR4 (unknown origin)	B	8.08	pIC50	8.3	nM	IC50	Eur J Med Chem (2024) 275: 116612-116612 [PMID:38908103]
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)
ChEMBL	Measurement of Inhibitory Effect on FGFR4 Kinase Activity: The inhibitory effect of the compounds on FGFR4 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FGFR4 protein was purchased from Carna Biosciences, Inc. The final concentration of ATP was 200 μM.	B	8.47	pIC50	3.4	nM	IC50	US-10894048-B2. Antitumor drug for intermittent administration of FGFR inhibitor (2021)
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 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]