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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
VEMURAFENIB

VEMURAFENIB


ATC L01EC01

ANTINEOPLASTIC AGENT
PROTEIN KINASE INHIBITOR
METASTATIC MELANOMA WITH BRAF-V600E MUTATION

ORAL

Cmax 126 MICROMOLAR (960 MILLIGRAM 15 DAYS)

VD 106 LITER

PPB 99 PERCENT

Cl 1.3 LITER / HOUR

HT 57 HOUR (960 MILLIGRAM)

SOLUBILITY PRACTICALLY INSOLUBLE IN AQUEOUS MEDIA

BRAF SERINE-THREONINE KINASE
CRAF
ARAF
SRMS
ACK1
MAP4K5
FGR

PDB 5HES (HUMAN LEUCINE ZIPPER- AND STERILE ALPHA MOTIF-CONTAINING KINASE (ZAK, MLT, HCCS-4, MRK, AZK, MLTK) IN COMPLEX WITH VEMURAFENIB)

LIGAND CODE = 032 (link to the list of PDB complexes)

Download experimental 3D coordinates of 032 with added hydrogens

Serine,threonine-protein kinase B-raf UNIPROT P15056 BRAF

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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