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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
DABRAFENIB

DABRAFENIB


ATC L01XE23

ANTINEOPLASTIC
MELANOMA WITH BRAF V600E
INHIBITOR

ORAL

F 95 PERCENT

VD 70.3 LITER

PPB 99.7 PERCENT

Cl 25.7 LITER / HOUR

HT 8 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE ABOVE PH 4

BRAF V600E KINASE (IC50=0.65 NANOMOLAR)
BRAF V600K (IC50=0.5 NANOMOLAR)
BRAF V600D (IC50=1.84 NANOMOLAR)
WILD-TYPE BRAF (3.2 NANOMOLAR)
CRAF KINASE (5 NANOMOLAR)

PDB 5CSW (B-RAF IN COMPLEX WITH DABRAFENIB)

LIGAND CODE = P06 (link to the list of PDB complexes)

Download experimental 3D coordinates of P06 with added hydrogens

SERINE/THREONINE-PROTEIN KINASE B-RAF INHIBITOR CHEMBL5145 SERINE/THREONINE-PROTEIN KINASE B-RAF P15056 SERINE/THREONINE-PROTEIN KINASE B-RAF HOMO SAPIENS ENZYME KINASE PROTEIN KINASE TKL RAFEMA

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