BDBM50428286 DABRAFENIB::GSK2118436A

SMILES CC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F

InChI Key InChIKey=BFSMGDJOXZAERB-UHFFFAOYSA-N

Data  25 IC50  4 EC50

PDB links: 6 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 29 hits for monomerid = 50428286   

TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  6nMAssay Description:Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogueMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of N-terminal His-tagged human B-Raf kinase domain (448 to 723 residues) expressed in Escherichia coli BL21 (DE3) by Lanthascreen assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  11nMAssay Description:Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  9.70nMAssay Description:Inhibition of wild type BRAF (unknown origin) assessed as ADP formation measured for 5 hrs by pyruvate kinase/lactate dehydrogenase coupled assay in ...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase A-Raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  26nMAssay Description:Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of wild type B-Raf (unknown origin) assessed as MEK1 phosphorylation using MEK1-Avitag as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataEC50:  529nMAssay Description:Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot methodMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  1nMAssay Description:Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot methodMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  1nMAssay Description:Inhibition of B-Raf V600E mutant (unknown origin) assessed as MEK1 phosphorylation using MEK1-Avitag as substrate after 1 hr by HTRF assayMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  3.70E+3nMAssay Description:Inhibition of Alk5 in TGF-beta-stimulated human HepG2 cells assessed as decrease in Smad2 phosphorylation treated for 45 mins prior to TGF-beta stimu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHeat shock factor protein 1(Homo sapiens (Human))
The Institute Of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHeat shock factor protein 1(Homo sapiens (Human))
The Institute Of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50: <1.00E+4nMAssay Description:Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  4nMAssay Description:Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by Western blot analysisMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of BRAF V600E mutant (unknown origin)More data for this Ligand-Target Pair
TargetPirin(Homo sapiens (Human))
The Institute Of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50: >1.00E+4nMAssay Description:Displacement of 6-amino-9-(2-((4-((2-((6-((5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)carbamoyl)quinolin-2-yl)oxy)ethyl)amino)-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50: <1nMAssay Description:Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression systemMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  5nMAssay Description:Inhibition of recombinant human full length GST-tagged BRAF expressed in baculovirus expression systemMore data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 3(Homo sapiens (Human))
Fudan University

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  2nMAssay Description:Inhibition of human RIPK3 using MBP as substrate by [gamma33-ATP] based radiometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual serine/threonine and tyrosine protein kinase(Homo sapiens (Human))
Fudan University

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  2.94E+4nMAssay Description:Inhibition of human RIPK5 using MBP as substrate by [gamma33-ATP] based radiometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Fudan University

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  5.32E+4nMAssay Description:Inhibition of human RIPK1 using MBP as substrate by [gamma33-ATP] based radiometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 3(Homo sapiens (Human))
Fudan University

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  250nMAssay Description:Inhibition of human full length N-terminal GST-tagged RIPK3 expressed in baculovirus infected sf9 insect cells assessed as reduction in MBP phosphory...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 2(Homo sapiens (Human))
Fudan University

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  77nMAssay Description:Inhibition of human RIPK2 using MBP as substrate by [gamma33-ATP] based radiometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of BRAF V600E mutant (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of BRAF V600E mutant (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of BRAF V600E mutant (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataEC50:  0.700nMAssay Description:Inhibition of N-terminal His-tagged human recombinant B-Raf V600E mutant (448 to 723 residues) expressed in Escherichia coli BL21 (DE3) by Lanthascre...More data for this Ligand-Target Pair
TargetNuclear receptor subfamily 1 group I member 2(Homo sapiens (Human))
Cnrs

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataEC50:  87nMAssay Description:Transactivation of Gal4-tagged human PXR transfected in human HeLa cells preincubated for 16 hrs followed by luciferin addition and measured after 10...More data for this Ligand-Target Pair
TargetNuclear receptor subfamily 1 group I member 2(Homo sapiens (Human))
Cnrs

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataEC50:  87nMAssay Description:Agonist activity at PXR (unknown origin)More data for this Ligand-Target Pair
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50428286(DABRAFENIB | GSK2118436A)
Affinity DataIC50:  150nMAssay Description:Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank