BDBM50531540 CHEBI:75998::GSK-1120212::GSK1120212::JTP 74057::JTP-74057::Mekinist::TMT-212::Tmt212::Trametinib::US11147816, Trametinib::US11701360, Trametinib

SMILES CC(=O)Nc1cccc(c1)-n1c2c(C)c(=O)n(C)c(Nc3ccc(I)cc3F)c2c(=O)n(C2CC2)c1=O

InChI Key InChIKey=LIRYPHYGHXZJBZ-UHFFFAOYSA-N

Data  10 IC50  1 EC50

PDB links: 3 PDB IDs match this monomer.

  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 11 hits for monomerid = 50531540   

TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Rheinische Friedrich-Wilhelms-University Of Bonn

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataEC50:  247nMAssay Description:Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 2(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  15nMAssay Description:Inhibition of MEK2 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  2.16nMAssay Description:The IC50 for MEK1 and 2 can be measured by methods in references such as [Yamaguchi et al. (2011) International Journal of Oncology 39:23-31].More data for this Ligand-Target Pair
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
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
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  2nMAssay Description:Inhibition of MEK 1/2 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  0.920nMAssay Description:Non competitive inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 2(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  1.80nMAssay Description:Non competitive inhibition of MEK2 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  0.920nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 2(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of MEK2 (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  2.16nMAssay Description:TBDMore data for this Ligand-Target Pair