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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
TRAMETINIB

TRAMETINIB


ATC L01EE01

ANTINEOPLASTIC
KINASE INHIBITOR
METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS

ORAL

F 72 PERCENT

VD 214 LITER

PPB 97.4 PERCENT

Cl 4.9 LITER / HOUR

HT 4.35 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE IN THE PH RANGE OF 2 TO 8 IN WATER

MEK1
MEK2

PDB 7JUR (CRYSTAL STRUCTURE OF KSR2:MEK1 IN COMPLEX WITH AMP-PNP AND ALLOSTERIC MEK INHIBITOR TRAMETINIB)

LIGAND CODE = QOM (link to the list of PDB complexes)

Download experimental 3D coordinates of QOM with added hydrogens

Dual specificity mitogen-activated protein kinase kinase 1 UNIPROT Q02750 MAP2K1 -- Dual specificity mitogen-activated protein kinase kinase 2 UNIPROT P36507 MAP2K2

more at DrugCentral

EMA

ANSM (in French)

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SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
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