ChEMBL ligand: CHEMBL1738797 (CH-5424802, Alectinib, AF-802, RO-5424802, Alecensa, RO5424802)
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!
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] 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!
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] 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!
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
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL	Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay	B	7.72	pIC50	19	nM	IC50	Eur. J. Med. Chem. (2016) 118: 244-249 [PMID:27131066]
ChEMBL	Inhibition of gatekeeper ALK L1196M mutant (unknown origin) using poly (Glu, Tyr)4:1 substrate incubated for 60 mins by ELISA	B	7.82	pIC50	15.2	nM	IC50	Eur. J. Med. Chem. (2015) 105: 39-56 [PMID:26476749]
ChEMBL	Inhibition of recombinant ALK (unknown origin) using poly (Glu, Tyr)4:1 substrate incubated for 60 mins by ELISA	B	7.94	pIC50	11.5	nM	IC50	Eur. J. Med. Chem. (2015) 105: 39-56 [PMID:26476749]
ChEMBL	Inhibition Assay: ALK-inhibiting activity was measured by following an activity of inhibiting phosphorylation by biotinylated peptide (EGPWLEEEEEAYGWMDF). For the detection of phosphorylation of the biotinylated peptide, time-resolved fluorescence measurement was performed using an anti-phosphorylated tyrosine antibody labeled with europium cryptate and streptavidin conjugated to XL665, i.e., an allophycocyanin derivative.	B	8.28	pIC50	5.3	nM	IC50	US-9126931-B2. Tetracyclic compound (2015)
GtoPdb	-	-	8.72	pIC50	1.9	nM	IC50	Bioorg. Med. Chem. (2012) 20: 1271-80 [PMID:22225917]
ChEMBL	Inhibition of ALK using Bio-Gastrintide as substrate by TR-FRET assay in presence of 30 uM of ATP	B	8.72	pIC50	1.9	nM	IC50	Bioorg. Med. Chem. (2012) 20: 1271-1280 [PMID:22225917]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
GtoPdb	-	-	5.3	pIC50	>5000	nM	IC50	Bioorg. Med. Chem. (2012) 20: 1271-80 [PMID:22225917]
ChEMBL	Inhibition of MET using Bio-HER2tide as substrate by TR-FRET assay in presence of 50 uM of ATP	B	5.3	pIC50	>5000	nM	IC50	Bioorg. Med. Chem. (2012) 20: 1271-1280 [PMID:22225917]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of human ERG	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2016) 26: 5399-5402 [PMID:27769623]
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 of ROS1 G2032R mutant (unknown origin)	B	5.52	pKi	>3000	nM	Ki	Eur J Med Chem (2017) 134: 348-356 [PMID:28431340]
ChEMBL	Inhibition of wild type ROS1 (unknown origin)	B	5.62	pKi	2400	nM	Ki	Eur J Med Chem (2017) 134: 348-356 [PMID:28431340]
ChEMBL	Inhibition of ROS1 L2026M mutant (unknown origin)	B	5.7	pKi	2000	nM	Ki	Eur J Med Chem (2017) 134: 348-356 [PMID:28431340]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL	Inhibition of KIT using Bio-HER2tide as substrate by TR-FRET assay in presence of 50 uM of ATP	B	5.3	pIC50	>5000	nM	IC50	Bioorg. Med. Chem. (2012) 20: 1271-1280 [PMID:22225917]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL	Inhibition of recombinant human RET V804M mutant using Biotin-EGPWLEEEEEAYGWMDF as substrate incubated for 60 mins by TR-FRET assay	B	7.4	pIC50	39.8	nM	IC50	Eur. J. Med. Chem. (2016) 118: 244-249 [PMID:27131066]
ChEMBL	Inhibition of wild type recombinant human RET using Biotin-EGPWLEEEEEAYGWMDF as substrate incubated for 60 mins by TR-FRET assay	B	8.32	pIC50	4.8	nM	IC50	Eur. J. Med. Chem. (2016) 118: 244-249 [PMID:27131066]
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 KDR using Bio-Gastrintide as substrate by TR-FRET assay in presence of 50 uM of ATP	B	5.85	pIC50	1400	nM	IC50	Bioorg. Med. Chem. (2012) 20: 1271-1280 [PMID:22225917]

ChEMBL data shown on this page come from version 27:

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]