BDBM50363397 CHEMBL1946170::REGORAFENIB::US10183928, Regorafenib::US10202365, Compound Regorafenib::US10227329, Compound Regorafenib::US10464902, Regorafenib::US10584114, Compound Regorafenib::US10774070, Compound Regorafenib::US11279688, Compound Regorafenib
SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)c(F)c2)ccn1
InChI Key InChIKey=FNHKPVJBJVTLMP-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 49 hits for monomerid = 50363397
Affinity DataKi: 4.20nMAssay Description:Compounds 2-4 and cabozantinib were each tested for binding of c-Met, VEGFR2, TIE2 and the control compound, staurosporine. Specifically, each compou...More data for this Ligand-Target Pair
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Homo sapiens (Human))
Federal University Of Parana
Curated by ChEMBL
Federal University Of Parana
Curated by ChEMBL
Affinity DataIC50: 3.00E+3nMAssay Description:Inhibition of ABCG2 (unknown origin) expressed in human S1M180 cells mediated [3H]-mitoxantrone efflux assessed as intracellular [3H]-mitoxantrone le...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
The Institute Of Cancer Research
Curated by ChEMBL
The Institute Of Cancer Research
Curated by ChEMBL
Affinity DataIC50: 28nMAssay Description:Inhibition of wild-type B-RafMore data for this Ligand-Target Pair
TargetBifunctional epoxide hydrolase 2(Homo sapiens (Human))
University Of California
Curated by ChEMBL
University Of California
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human recombinant soluble epoxide hydrolase assessed as cyano(6-methoxy-naphthalen-2-yl)methyl trans-[(3-phenyloxyran-2-yl)methyl] carb...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 5.10nMAssay Description:A compound described herein can be tested in vitro for inhibition of wild-type RET and various mutant RET kinases, including e.g., RET V804L, RET V80...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 29.8nMAssay Description:A compound described herein can be tested in vitro for inhibition of wild-type RET and various mutant RET kinases, including e.g., RET V804L, RET V80...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 5.10nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 29.8nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 46.7nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 5.10nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 29.8nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 46.7nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...More data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Tu Dortmund University
Curated by ChEMBL
Tu Dortmund University
Curated by ChEMBL
Affinity DataIC50: 6.10nMAssay Description:Concentration required to inhibit the activity of K+ stimulated gastric ATPaseMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 12nMAssay Description:In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 53nMAssay Description:In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 1(Homo sapiens (Human))
Fuzhou University
Curated by ChEMBL
Fuzhou University
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Inhibition of VEGFR1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.20nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 5.10nMAssay Description:In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 29.8nMAssay Description:In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 46.7nMAssay Description:In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...More data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Tu Dortmund University
Curated by ChEMBL
Tu Dortmund University
Curated by ChEMBL
Affinity DataIC50: 116nMAssay Description:Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovir...More data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
National Health Research Institutes
Curated by ChEMBL
National Health Research Institutes
Curated by ChEMBL
Affinity DataIC50: 82nMAssay Description:Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using...More data for this Ligand-Target Pair
Affinity DataIC50: 4.20nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of GST-tagged TIE2 (unknown origin) using biotin-Ahx-EPKDDAYPLYSDFG peptide as substrate by HTRF methodMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
The Institute Of Cancer Research
Curated by ChEMBL
The Institute Of Cancer Research
Curated by ChEMBL
Affinity DataIC50: 40nMAssay Description:Inhibition of human wild type BRAF by Kinase-Glo luminescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description: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 AT...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Mus musculus)
National Research Centre
Curated by ChEMBL
National Research Centre
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of mouse VEGFR-2 (785 to 1376 residues)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 1(Homo sapiens (Human))
Fuzhou University
Curated by ChEMBL
Fuzhou University
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of VEGFR1 (unknown origin)More data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor beta(Homo sapiens (Human))
National Research Centre
Curated by ChEMBL
National Research Centre
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of PDGFR beta (561 to 1106 residues) (unknown origin)More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
National Research Centre
Curated by ChEMBL
National Research Centre
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of FGFR1 (unknown origin)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 3(Mus musculus (mouse))
National Research Centre
Curated by ChEMBL
National Research Centre
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of mouse VEGFR-3 (818 to 1363 residues)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
The Institute Of Cancer Research
Curated by ChEMBL
The Institute Of Cancer Research
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of BRAF (unknown origin)More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
National Research Centre
Curated by ChEMBL
National Research Centre
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of RAF1 (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 12nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 53nMAssay Description:In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of VEGFR 2 (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 1.5nMAssay Description:Inhibition of human RET kinase using IGF1Rtide as substrate incubated for 40 mins and measured by ADP-Glo assayMore data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
National Research Centre
Curated by ChEMBL
National Research Centre
Curated by ChEMBL
Affinity DataIC50: 2.5nMAssay Description:Inhibition of RAF1 (305 to 648 residues) (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
The Institute Of Cancer Research
Curated by ChEMBL
The Institute Of Cancer Research
Curated by ChEMBL
Affinity DataIC50: 19nMAssay Description:Inhibition of BRAF V600E (409 to 765 residues) (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Blueprint Medicines
US Patent
Blueprint Medicines
US Patent
Affinity DataIC50: 1.5nMAssay Description:Inhibition of RET (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
The Institute Of Cancer Research
Curated by ChEMBL
The Institute Of Cancer Research
Curated by ChEMBL
Affinity DataIC50: 28nMAssay Description:Inhibition of BRAF (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 1(Homo sapiens (Human))
Fuzhou University
Curated by ChEMBL
Fuzhou University
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Inhibition of VEGFR1 (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4.20nMAssay Description:Inhibition of VEGFR2 (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 3(Homo sapiens (Human))
University Of Arkansas For Medical Sciences
Curated by ChEMBL
University Of Arkansas For Medical Sciences
Curated by ChEMBL
Affinity DataIC50: 46nMAssay Description:Inhibition of VEGFR3 (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
National Research Centre
Curated by ChEMBL
National Research Centre
Curated by ChEMBL
Affinity DataIC50: 202nMAssay Description:Inhibition of FGFR1 (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Tu Dortmund University
Curated by ChEMBL
Tu Dortmund University
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of c-kit (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 311nMAssay Description:Inhibition of Tie-2 (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
Affinity DataKd: 869nMAssay Description:Kinobeads competition assays were performed in 96-well format as previously described using mixed protein lysates of four cancer cell lines (K-562, M...More data for this Ligand-Target Pair
TargetGlycine receptor subunit alpha-1(Homo sapiens (Human))
University Of Pittsburgh
Curated by ChEMBL
University Of Pittsburgh
Curated by ChEMBL
Affinity DataEC50: 1.80E+3nMAssay Description:Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-el...More data for this Ligand-Target Pair