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.

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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 18 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 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
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
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
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