delgocitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Janus kinase inhibitors, antineoplastics 5426 1263774-59-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • delgocitinib
  • JTE-052
  • JTE-052A
  • LEO 124249
  • LEO 124249A
  • LP0133
  • corectim
Delgocitinib, a janus kinase (JAK) inhibitor, is being approved for the treatment of inflammatory skin conditions. Delgocitinib inhibited the activation of inflammatory cells, such as T cells, B cells, monocytes and mast cells, in vitro and inhibited Th1-, Th2- and Th17-type cytokine production from both T cells and non-T cells.
  • Molecular weight: 310.36
  • Formula: C16H18N6O
  • CLOGP: 1
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 88.91
  • ALOGS: -2.75
  • ROTB: 2

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 23, 2020 PMDA Japan Tobacco

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
CHEBI has role CHEBI:35472 anti-inflammatory drugs
CHEBI has role CHEBI:50748 antipsoriatic drug
CHEBI has role CHEBI:59010 antiseborrheics
CHEBI has role CHEBI:76617 BTK inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Atopic dermatitis indication 24079001 DOID:3310




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 7.89 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 8.55 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 8.58 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 7.24 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase Lck Kinase IC50 5.24 CHEMBL
Rho-associated protein kinase 2 Kinase INHIBITOR IC50 6.58 SCIENTIFIC LITERATURE

External reference:

IDSource
D11046 KEGG_DRUG
9L0Q8KK220 UNII
C5226741 UMLSCUI
CHEBI:167600 CHEBI
FHX PDB_CHEM_ID
CHEMBL4297507 ChEMBL_ID
50914062 PUBCHEM_CID
DB16133 DRUGBANK_ID
9619 IUPHAR_LIGAND_ID
C000621572 MESH_SUPPLEMENTAL_RECORD_UI
10574 INN_ID

Pharmaceutical products:

None