BDBM50363397 CHEMBL1946170::REGORAFENIB::US10183928, Regorafenib::US10202365, Compound Regorafenib::US10227329, Compound Regorafenib::US10464902, Regorafenib::US10584114, Compound Regorafenib::US10774070, Compound Regorafenib::US11279688, Compound Regorafenib::US11912663, Compound Regorafenib::US12071408, Example 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 90 hits for monomerid = 50363397
Affinity DataIC50: 10nMAssay Description:In this experiment, the inhibitory effects of small molecule inhibitors on 17 kinases were examined by using fluorescent microfluidic mobility shift ...More data for this Ligand-Target Pair
Affinity DataIC50: 158nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 34nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 55nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 500nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 1.50E+3nMAssay Description:Inhibition of KIT (delta 560 to 576 residues) deletion/V654A double mutant autophosphorylation at Y703 in human GIST-430/654 harboring KIT (delta 560...More data for this Ligand-Target Pair
Affinity DataIC50: 131nMAssay Description:Inhibition of KIT (delta560 to 576 residues) deletion mutant autophosphorylation at Y703 in human GIST430 harboring KIT (delta560 to 576 residues) de...More data for this Ligand-Target Pair
Affinity DataIC50: 280nMAssay Description:Inhibition of KIT V654A mutant (unknown origin) by FRET based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4.20nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 2(Human)
University of Lille
Curated by ChEMBL
University of Lille
Curated by ChEMBL
Affinity DataIC50: 41nMAssay Description:Inhibition of human RIPK2 (8 to 317 residues) expressed in Sf9 cells in presence of ATP by ADP Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.70E+4nMAssay Description:Stabilized cells were dropped onto circular slides and placed in a culture dish with a cell density below 50% and incubated overnight. Cells for expe...More data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 7.5nMAssay Description:In this experiment, the inhibitory effects of small molecule inhibitors on 17 kinases were examined by using fluorescent microfluidic mobility shift ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:In this experiment, the inhibitory effects of small molecule inhibitors on 17 kinases were examined by using fluorescent microfluidic mobility shift ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:In this experiment, the inhibitory effects of small molecule inhibitors on 17 kinases were examined by using fluorescent microfluidic mobility shift ...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:In this experiment, the inhibitory effects of small molecule inhibitors on 17 kinases were examined by using fluorescent microfluidic mobility shift ...More data for this Ligand-Target Pair
Affinity DataIC50: 42nMAssay Description:Inhibition of VEGFR3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.60nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of VEGFR1 (unknown origin)More data for this Ligand-Target Pair
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(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
Affinity DataIC50: 311nMAssay Description:Inhibition of Tie-2 (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of c-kit (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha(Human)
Iran University of Medical Sciences
Curated by ChEMBL
Iran University of Medical Sciences
Curated by ChEMBL
TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
TargetVascular endothelial growth factor receptor 3(Mouse)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
TargetVascular endothelial growth factor receptor 2(Mouse)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 202nMAssay Description:Inhibition of FGFR1 (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 3(Mouse)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
TargetVascular endothelial growth factor receptor 2(Mouse)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 1.00E+3nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+3nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha(Human)
Iran University of Medical Sciences
Curated by ChEMBL
Iran University of Medical Sciences
Curated by ChEMBL
Affinity DataIC50: 16nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 12nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 500nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
Affinity DataIC50: 62nMAssay Description:1. Buffer configuration: 50 mM HEPES, pH 7.5, 0.00015% Brij-35.2. Compounds were configured in 100% DMSO in a concentration gradient and diluted with...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](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
TargetReceptor-type tyrosine-protein kinase FLT3(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: 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
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](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
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](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