BDBM202780 US10245267, Example 127::US10709712, Example 127::US9242969, 127::US9694016, 127

SMILES COc1ncc(cc1N1CCOCC1)-c1cc(NC(=O)c2cccc(c2)C(F)(F)F)cnc1C

InChI Key InChIKey=BSUIIPUXGLKINZ-UHFFFAOYSA-N

Data  16 IC50  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 17 hits for monomerid = 202780   

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.310nMAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2× final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.400nMAssay Description:C-Raf TR refers to a truncated C-Raf protein, a Δ1-324 deletion mutant.C-Raf FL refers to the full-length C-Raf protein.Full length MEK1 with an...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2021
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 1.90nMAssay Description:C-Raf TR refers to a truncated C-Raf protein, a Δ1-324 deletion mutant.C-Raf FL refers to the full-length C-Raf protein.Full length MEK1 with an...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2021
Entry Details
Go to US Patent

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.310nMAssay Description:C-Raf TR refers to a truncated C-Raf protein, a Δ1-324 deletion mutant.C-Raf FL refers to the full-length C-Raf protein.Full length MEK1 with an...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2021
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 1.67nMAssay Description:C-Raf TR refers to a truncated C-Raf protein, a Δ1-324 deletion mutant.C-Raf FL refers to the full-length C-Raf protein.Full length MEK1 with an...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2021
Entry Details
Go to US Patent

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.760nMAssay Description:C-Raf TR refers to a truncated C-Raf protein, a Δ1-324 deletion mutant.C-Raf FL refers to the full-length C-Raf protein.Full length MEK1 with an...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2021
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 2.75nMAssay Description:C-Raf TR refers to a truncated C-Raf protein, a Δ1-324 deletion mutant.C-Raf FL refers to the full-length C-Raf protein.Full length MEK1 with an...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2021
Entry Details
Go to US Patent

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.400nMAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2× final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 1.90nMAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2× final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf(Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 1.67nMpH: 7.5 T: 2°CAssay Description:Final assay conditions were 4 pM cRaf, 3 uM ATP, 10 nM biotin tagged MEK1 kinase dead protein substrate. Reactions were performed in Greiner384 well ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 1.67nMAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2× final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataEC50:  250nMAssay Description:Inhibition CRAF in human Calu6 cells assessed as decrease in MEK phosphorylation after 2 hrs by HTRF methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2019
Entry Details Article
PubMed
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.310nMpH: 7.5 T: 2°CAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2x final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/19/2018
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 1.67nMpH: 7.5 T: 2°CAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2x final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/19/2018
Entry Details
Go to US Patent

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.400nMpH: 7.5 T: 2°CAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2x final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/19/2018
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase B-raf [V600E](Human)
Novartis

US Patent
LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 1.90nMpH: 7.5 T: 2°CAssay Description:Raf and biotinylated Mek, kinase dead, were combined at 2x final concentrations in assay buffer (50 mM Tris, pH 7.5, 15 mM MgCl2, 0.01% BSA and 1 mM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/19/2018
Entry Details
Go to US Patent

LigandPNGBDBM202780(US9694016, 127 | US9242969, 127 | US10245267, Exam...)
Affinity DataIC50: 0.310nMpH: 7.5 T: 2°CAssay Description:Final assay conditions were 4 pM cRaf, 3 uM ATP, 10 nM biotin tagged MEK1 kinase dead protein substrate. Reactions were performed in Greiner384 well ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details
Go to US Patent