ChEMBL ligand: CHEMBL3301622 (Asp-2215, ASP2215, ASP-2215, Gilteritinib)
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] There should be some charts here, you may need to enable JavaScript!
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] There should be some charts here, you may need to enable JavaScript!
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] There should be some charts here, you may need to enable JavaScript!
neurotrophic receptor tyrosine kinase 1 in Human [GtoPdb: 1817] [UniProtKB: P04629] There should be some charts here, you may need to enable JavaScript!
MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866] There should be some charts here, you may need to enable JavaScript!
leukocyte receptor tyrosine kinase in Human [GtoPdb: 1838] [UniProtKB: P29376] 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
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL	Inhibition Assay: A recombinant retrovirus was created from expression plasmid FLAG-EML4-ALKv1/pMX-iresCD8 in which cDNA for EMLA-ALK fusion protein v1 was integrated, and injected into mouse lymphoid cell line BA/F3 cells. Using a magnetic bead reagent for cell separation and a purification column (anti-CD8 monoclonal antibody immobilized on magnetic beads and a MiniMACS purification column; both are products of MilteDyi Biotec Inc.), cell surface CD8-expressing cells were purified to establish EML4-ALK fusion protein v1-expressing BA/F3 cells. From the cells, EML4-ALK fusion protein v1 was purified and subjected to kinase activity evaluation. EML4-ALK fusion protein v1 was investigated for its phosphorylation activity toward a peptide substrate by using a kinase activity detection kit (HTRF KinEASE-TK; Cisbio Inc.). Test compounds were each added to a reaction solution containing the enzyme protein to give 8 final concentrations from 1000 nM to 0.3 nM, followed by addition of ATP.	B	8.82	pIC50	1.5	nM	IC50	US-8969336-B2. Diamino heterocyclic carboxamide compound (2015)
GtoPdb	-	-	9.3	pIC50	~0.5	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
ChEMBL	Inhibition Assay: A partial protein of only a kinase domain of ROS protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Example 5, except that the ATP concentration in the mixed solution of ATP and substrate peptide (Caliper) was 50 uM. Test Example 5: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition.	B	8.72	pIC50	1.9	nM	IC50	US-8969336-B2. Diamino heterocyclic carboxamide compound (2015)
GtoPdb	-	-	8.82	pIC50	~1.5	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL	Inhibition Assay: A partial protein of only a kinase domain of FLT3 protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Example 5. Test Example 5: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition.	B	9.39	pIC50	0.41	nM	IC50	US-8969336-B2. Diamino heterocyclic carboxamide compound (2015)
GtoPdb	-	-	9.52	pIC50	~0.3	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]
ChEMBL	Inhibition of N-terminal GST-tagged human FLT3 (564 to 993 residues) cytoplasmic domain expressed in baculovirus expression system by ELISA	B	9.54	pIC50	0.29	nM	IC50	Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL	Inhibition Assay: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition. In the absence of the test compound, the phosphorylation peptide peak without ATP addition and with ATP addition was assumed to be 100% inhibition and 0% inhibition, respectively.	B	8.47	pIC50	3.4	nM	IC50	US-8969336-B2. Diamino heterocyclic carboxamide compound (2015)
GtoPdb	-	-	8.77	pIC50	~1.7	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL	Inhibition of AXL (unknown origin) using poly (Glu, Tyr) as substrate after 60 mins by ELISA	B	7.95	pIC50	11.3	nM	IC50	Bioorg Med Chem Lett (2019) 29: 836-838 [PMID:30685094]
ChEMBL	Inhibition of AXL (unknown origin)	B	9	pIC50	<1	nM	IC50	J. Med. Chem. (2016) 59: 3593-3608 [PMID:26555154]
GtoPdb	-	-	9.1	pIC50	~0.8	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]
ChEMBL	Inhibition of N-terminal GST-tagged human AXL (464 to 885 residues) cytoplasmic domain expressed in baculovirus expression system by ELISA	B	9.14	pIC50	0.73	nM	IC50	Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
neurotrophic receptor tyrosine kinase 1 in Human [GtoPdb: 1817] [UniProtKB: P04629]
GtoPdb	-	-	8.96	pIC50	~1.1	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]
MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866]
GtoPdb	-	-	8.52	pIC50	~3	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]
leukocyte receptor tyrosine kinase in Human [GtoPdb: 1838] [UniProtKB: P29376]
GtoPdb	-	-	9.7	pIC50	~0.2	nM	IC50	Blood (2017) 129: 257-260 [PMID:27908881]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]