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| 1 | INN | Class | Route (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 complex | Targets from DrugCentral | Links | |||
| M SELUMETINIB (is an active metabolite)
| SELUMETINIB | ANTINEOPLASTIC | - | MEK1 MEK2 | 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 | ||||
| 2 | INN | Class | Route (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 complex | Targets from DrugCentral | Links | |||
| SELUMETINIB (has an active metabolite)
| SELUMETINIB | ANTINEOPLASTIC | ORAL | Cmax 1.74 MICROMOLAR Tmax 1.25 HOUR F 62 PERCENT VD 171 LITER PPB 98.4 PERCENT Cl 8.8 LITER / HOUR HT 6.2 HOUR SOLUBILITY SLIGHTLY SOLUBLE AT PH > 3 | MEK1 MEK2 PDB 4U7Z (MITOGEN-ACTIVATED PROTEIN KINASE KINASE (MEK1) BOUND TO G805) LIGAND CODE = 3EW (link to the list of PDB complexes) Download experimental 3D coordinates of 3EW 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 | |||
