azimilide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
class III antiarrhythmics, sematilide derivatives 274 149908-53-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • azimilide hydrochloride
  • azimilide dihydrochloride
  • azimilide
  • azimilide HCl
  • Molecular weight: 457.96
  • Formula: C23H28ClN5O3
  • CLOGP: 2.35
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 0
  • TPSA: 72.60
  • ALOGS: -3.73
  • ROTB: 8

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 13 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.06 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 79 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.74 Basic
pKa2 4.74 Basic
pKa3 0.93 Basic

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
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.40 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.74 CHEMBL
Potassium voltage-gated channel subfamily KQT member 1 Ion channel IC50 6.62 CHEMBL
Potassium voltage-gated channel subfamily KQT member 1 Ion channel BLOCKER IC50 5.30 IUPHAR

External reference:

IDSource
D03037 KEGG_DRUG
149888-94-8 SECONDARY_CAS_RN
C0252416 UMLSCUI
CHEBI:34545 CHEBI
CHEMBL123558 ChEMBL_ID
CHEMBL3140370 ChEMBL_ID
CHEMBL537847 ChEMBL_ID
DB04957 DRUGBANK_ID
C086123 MESH_SUPPLEMENTAL_RECORD_UI
2588 IUPHAR_LIGAND_ID
7299 INN_ID
74QU6P2934 UNII
9571004 PUBCHEM_CID

Pharmaceutical products:

None