merestinib [Ligand Id: 9841] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3545307 (Ly-2801653, Merestinib, LY-2801653, LY2801653)
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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  • fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888]
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  • MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866]
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  • tyrosine kinase with immunoglobulin like and EGF like domains 1 in Human [GtoPdb: 1841] [UniProtKB: P35590]
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  • TEK receptor tyrosine kinase in Human [GtoPdb: 1842] [UniProtKB: Q02763]
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  • discoidin domain receptor tyrosine kinase 1 in Human [GtoPdb: 1843] [UniProtKB: Q08345]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
GtoPdb - - 8.7 pKi 2 nM Ki Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
ChEMBL Inhibition of cMET (unknown origin) by FISH assay B 8.33 pIC50 4.7 nM IC50 J Med Chem (2019) 62: 1731-1760 [PMID:30188734]
GtoPdb Inhibition of in vitro biochemical activity by EMD Millipore assay. - 8.33 pIC50 4.7 nM IC50 Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
GtoPdb Inhibition of in vitro biochemical activity by EMD Millipore assay. - 7.92 pIC50 12 nM IC50 Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
ChEMBL Inhibition of RON (unknown origin) by FISH assay B 8.92 pIC50 1.2 nM IC50 J Med Chem (2019) 62: 1731-1760 [PMID:30188734]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL Inhibition of MNK1 (unknown origin) B 6.89 pIC50 130 nM IC50 J Med Chem (2020) 63: 621-637 [PMID:31910010]
MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL Inhibition of MNK2 (unknown origin) B 6.96 pIC50 109 nM IC50 J Med Chem (2020) 63: 621-637 [PMID:31910010]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Inhibition of human full length AXL by scintillation counting method in presence of 33P-gammaATP B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2016) 59: 3593-3608 [PMID:26555154]
GtoPdb Inhibition of in vitro biochemical activity by EMD Millipore assay. - 7.96 pIC50 11 nM IC50 Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
ChEMBL Inhibition of human full length AXL after 4 hrs followed by stimulation with human recombinant Gas6 for 15 minutes by cell based assay B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2016) 59: 3593-3608 [PMID:26555154]
fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888]
GtoPdb Inhibition of in vitro biochemical activity by EMD Millipore assay. - 7.51 pIC50 31 nM IC50 Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866]
GtoPdb Binding constant determined by KINOMEScan assay. - 9.1 pKd 0.8 nM Kd Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
tyrosine kinase with immunoglobulin like and EGF like domains 1 in Human [GtoPdb: 1841] [UniProtKB: P35590]
GtoPdb Binding constant assessed by KINOMEScan assay. - 9.05 pKd 0.9 nM Kd Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
TEK receptor tyrosine kinase in Human [GtoPdb: 1842] [UniProtKB: Q02763]
GtoPdb Inhibition of in vitro biochemical activity by EMD Millipore assay. - 8.4 pIC50 4 nM IC50 Invest New Drugs (2013) 31: 833-44 [PMID:23275061]
discoidin domain receptor tyrosine kinase 1 in Human [GtoPdb: 1843] [UniProtKB: Q08345]
GtoPdb Binding constant determined by KINOMEScan assay. - 9.02 pKd 0.95 nM Kd Invest New Drugs (2013) 31: 833-44 [PMID:23275061]

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, 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]