BDBM87998 US10245267, Example 1029::US10709712, Example 1030::US9694016, 1029

SMILES Cc1ncc(NC(=O)c2cccc(c2)C(F)(F)F)cc1-c1cnc(O[C@H]2CCOC[C@H]2F)c(c1)N1CCOCC1

InChI Key InChIKey=HVTUZZBOLLPTQC-UHFFFAOYSA-N

Data  9 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 10 hits for monomerid = 87998   

TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
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
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 0.910nMAssay 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
US Patent

TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 1.56nMAssay 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
US Patent

TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 1.56nMAssay 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
US Patent

LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 1.56nMpH: 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
US Patent

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

US Patent
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 2.49nMAssay 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
US Patent

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

US Patent
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 3.27nMAssay 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
US Patent

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

US Patent
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 3.27nMAssay 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
US Patent

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

US Patent
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataIC50: 3.27nMpH: 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
US Patent

TargetRAF proto-oncogene serine/threonine-protein kinase(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM87998(US9694016, 1029 | US10245267, Example 1029 | US107...)
Affinity DataEC50:  5nMAssay Description:Inhibition of CRAF in human Calu6 cells assessed as reduction MEK phosphorylation measured after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed