regorafenib [Ligand Id: 5891] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1946170 (BAY-734506, Regorafenib, BAY 73-4506 monohydrate, BAY 73-4506, BAY-73-4506, Stivarga)
  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
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!
  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
There should be some charts here, you may need to enable JavaScript!
  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
There should be some charts here, you may need to enable JavaScript!
  • B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
There should be some charts here, you may need to enable JavaScript!
  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
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!
  • 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!
  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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]
  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Mouse [ChEMBL: CHEMBL3337] [GtoPdb: 1813] [UniProtKB: P35918]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Mouse [ChEMBL: CHEMBL4758] [GtoPdb: 1814] [UniProtKB: P35917]
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
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
ChEMBL Inhibition of human recombinant soluble epoxide hydrolase assessed as cyano(6-methoxy-naphthalen-2-yl)methyl trans-[(3-phenyloxyran-2-yl)methyl] carbonate conversion to 6-methoxy-2-naphthaldehyde preincubated for 5 mins prior to substrate addition by fluorescence assay B 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3732-3737 [PMID:23726028]
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 FGFR1 (unknown origin) B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
ChEMBL Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay B 5.74 pEC50 1800 nM EC50 J. Med. Chem. (2015) 58: 2958-2966 [PMID:25790278]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibition of PDGFR beta (561 to 1106 residues) (unknown origin) B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
ChEMBL Inhibition of human wild type BRAF by Kinase-Glo luminescence assay B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
GtoPdb - - 7.55 pIC50 28 nM IC50 Bioorg Med Chem Lett (2012) 22: 789-92 [PMID:22222036]
ChEMBL Inhibition of wild-type B-Raf B 7.55 pIC50 28 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 789-792 [PMID:22222036]
ChEMBL Inhibition of B-Raf V600E mutant B 7.72 pIC50 19 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 789-792 [PMID:22222036]
ChEMBL Inhibition of BRAF (unknown origin) B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Inhibition of RAF1 (unknown origin) B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
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 V559D/T670I double mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay B 5.67 pIC50 2153.3 nM IC50 J Med Chem (2017) 60: 8801-8815 [PMID:28991465]
ChEMBL Inhibition of KIT D816H mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay B 6.62 pIC50 239.1 nM IC50 J Med Chem (2017) 60: 8801-8815 [PMID:28991465]
ChEMBL Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of ATP by ADP-glo reagent based luminescence assay B 6.94 pIC50 116 nM IC50 J Med Chem (2019) 62: 11135-11150 [PMID:31721578]
ChEMBL Inhibition of wild type KIT (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay B 8.21 pIC50 6.1 nM IC50 J Med Chem (2017) 60: 8801-8815 [PMID:28991465]
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 of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based luminescence assay B 7.09 pIC50 82 nM IC50 J Med Chem (2019) 62: 11135-11150 [PMID:31721578]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of GST-tagged TIE2 (unknown origin) using biotin-Ahx-EPKDDAYPLYSDFG peptide as substrate by HTRF method B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of VEGFR1 (unknown origin) B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2019) 179: 916-935 [PMID:31306818]
ChEMBL Inhibition of VEGFR1 (unknown origin) B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
GtoPdb - - 7.9 pIC50 13 nM IC50 Int J Cancer (2011) 129: 245-55 [PMID:21170960]
ChEMBL Inhibition of human N-terminal GST tagged VEGFR-2 expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate in presence of ATP by Kinase-Glo luminescence assay B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 8.38 pIC50 4.2 nM IC50 Eur J Med Chem (2019) 179: 916-935 [PMID:31306818]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 8.38 pIC50 4.2 nM IC50 Eur J Med Chem (2019) 168: 315-329 [PMID:30826508]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3337] [GtoPdb: 1813] [UniProtKB: P35918]
ChEMBL Inhibition of mouse VEGFR-2 (785 to 1376 residues) B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4758] [GtoPdb: 1814] [UniProtKB: P35917]
ChEMBL Inhibition of mouse VEGFR-3 (818 to 1363 residues) B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 179: 707-722 [PMID:31284081]

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]