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ChEMBL ligand: CHEMBL1738797 (CH-5424802, Alectinib, AF-802, RO-5424802, Alecensa, RO5424802) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]