Affinity DataKi: 2.00E+3nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 8.00E+3nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 1.90E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 3.60E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 4.20E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 4.90E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 5.80E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
Affinity DataKi: 7.80E+4nMAssay Description:Covalent inhibition of human PRMT5 assessed as initial binding constant by LC-MS analysisMore data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.100nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of full-length BRAF (unknown origin)More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.600nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.700nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of MEK in human KYSE-520 cells assessed as reduction in p-ERK levelsMore data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.10nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 1.70nMAssay Description:Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate additio...More data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Inhibition of KRAS G12C mutant in human MIA PaCa-2 cells assessed as reduction in p-ERK levelsMore data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Allosteric inhibition of human SHP2 in human KYSE-520 cells assessed as reduction in ERK1/2 phosphorylation by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 12nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Allosteric inhibition of human SHP2 in human KYSE-520 cells assessed as reduction in ERK1/2 phosphorylation by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 14nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 15nMAssay Description:Inhibition of EGFR in human KYSE-520 cells assessed as reduction in p-ERK levelsMore data for this Ligand-Target Pair
In DepthDetails
Article
BindingDB Entry DOI: 10.7270/Q2CC14BBPubMedDrugBank
MMDB
PDB
3D Structure (crystal)
BindingDB Entry DOI: 10.7270/Q2CC14BBPubMedDrugBank
MMDB
PDB
![3D 3D](/images/Docked_3d.png)
Affinity DataIC50: 17nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 17nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Displacement of fluorescent tracer Rap-Gly-BDP from nanoluciferse-tagged human FKBP12 expressed in HEK293T cells incubated for 2 hrs by NanoBRET assa...More data for this Ligand-Target Pair
Affinity DataIC50: 22nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 23nMAssay Description:Displacement of fluorescent probe SLFb-2PEG-TAMRA from N-terminal 6His-SUMO-tagged human full length FKBP12 expressed in Escherichia coli BL21 (DE3) ...More data for this Ligand-Target Pair
Affinity DataIC50: 23nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 24nMAssay Description:Allosteric inhibition of human SHP2 in human KYSE-520 cells assessed as reduction in ERK1/2 phosphorylation by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 27nMAssay Description:Displacement of fluorescent probe SLFb-2PEG-TAMRA from N-terminal 6His-SUMO-tagged human full length FKBP12 expressed in Escherichia coli BL21 (DE3) ...More data for this Ligand-Target Pair
Affinity DataIC50: 28nMAssay Description:Allosteric inhibition of human SHP2 in human KYSE-520 cells assessed as reduction in ERK1/2 phosphorylation by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 29nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 29nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in p-ERK levelsMore data for this Ligand-Target Pair
Affinity DataIC50: 38nMAssay Description:Displacement of fluorescent probe SLFb-2PEG-TAMRA from N-terminal 6His-SUMO-tagged human full length FKBP12 expressed in Escherichia coli BL21 (DE3) ...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Allosteric inhibition of human SHP2 in human KYSE-520 cells assessed as reduction in ERK1/2 phosphorylation by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Displacement of fluorescent probe SLFb-2PEG-TAMRA from N-terminal 6His-SUMO-tagged human full length FKBP12 expressed in Escherichia coli BL21 (DE3) ...More data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Displacement of fluorescent probe SLFb-2PEG-TAMRA from N-terminal 6His-SUMO-tagged human full length FKBP12 expressed in Escherichia coli BL21 (DE3) ...More data for this Ligand-Target Pair
Affinity DataIC50: 58nMAssay Description:Displacement of fluorescent probe SLFb-2PEG-TAMRA from N-terminal 6His-SUMO-tagged human full length FKBP12 expressed in Escherichia coli BL21 (DE3) ...More data for this Ligand-Target Pair
Affinity DataIC50: 67nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 70nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
Affinity DataIC50: 70nMAssay Description:Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY...More data for this Ligand-Target Pair
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