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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
BELUMOSUDIL

BELUMOSUDIL


ATC L04AA48

ANTINEOPLASTIC
TREATMENT OF CHRONIC GRAFT-VERSUS-HOST DISEASE (GVHD)
RHO-ASSOCIATED COILED-COIL ROCK KINASE INHIBITOR (ROCK2 IC50= 100 NANOMOLAR
ROCK1 IC50=3 MICROMOLAR)

ORAL

Cmax 5.2 MICROMOLAR

Tmax 1.9 HOUR

F 64 PERCENT

VD 184 LITER

PPB 99.9 PERCENT

Cl 9.83 LITER / HOUR

HT 19 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE IN WATER

ROCK2 KINASE

PDB 7Z39 (STRUCTURE OF BELUMOSUDIL BOUND TO CK2ALPHA)

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

Download experimental 3D coordinates of ICQ with added hydrogens

Rho-associated protein kinase 1 UNIPROT Q13464 ROCK1 -- Rho-associated protein kinase 2 UNIPROT O75116 ROCK2

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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