ethacizine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
4835 33414-33-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ethacizine
  • ethacizine hydrochloride
  • etacizin
  • ethacizin
  • ethacizine HCl
  • Molecular weight: 413.54
  • Formula: C22H27N3O3S
  • CLOGP: 3.93
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 61.88
  • ALOGS: -4.64
  • ROTB: 8

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.592 Moderate 0.72
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.535 Moderate 0.72
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 25.235 10^-6 cm/s Moderate 0.72
dh-clint Dog hepatocyte intrinsic clearance 35.237 uL/min/10^6 cells Moderate 0.72
dppb Dog plasma protein binding (% unbound) 11.620 % Moderate 0.72
fcs-ppb Fetal calf serum protein binding (% unbound) 20.080 % Moderate 0.72
herg hERG pIC50 6.019 pIC50 Moderate 0.72
hh-clint Human hepatocyte intrinsic clearance 11.641 uL/min/10^6 cells Moderate 0.72
hlm-clint Human liver microsomal intrinsic clearance 47.098 uL/min/mg protein Moderate 0.72
hppb Human plasma protein binding (% unbound) 12.300 % Moderate 0.72
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 64
kinase-selectivity-class AXL,EIF2AK3,GRK2,PDK4,STK33,TEK 6
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 3.266 Moderate 0.72
mh-clint Mouse hepatocyte intrinsic clearance 185.780 Moderate 0.72
mppb Mouse plasma protein binding (% unbound) 17.280 Moderate 0.72
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 20.137 Moderate 0.72
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 19.350 % Moderate 0.72
rh-clint Rat hepatocyte intrinsic clearance 167.880 uL/min/10^6 cells Moderate 0.72
rh-fuinc Rat hepatocyte fraction unbound in incubation 46.270 % Moderate 0.72
rppb Rat plasma protein binding (% unbound) 12.890 % Moderate 0.72
solubility-dd Solubility at pH 7.4 in DMSO 907.821 uM Moderate 0.72

Approvals:

None

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
ATC C01BC09 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
ANTIARRHYTHMICS, CLASS I AND III
Antiarrhythmics, class Ic
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
CHEBI has role CHEBI:38070 anti-arrhythmia drug

Related Drugs by ATC class:

C01BC Antiarrhythmics, class Ic 4 drugs
encainideflecainidelorcainidepropafenone

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

DiseaseRelationSNOMED_IDDOID
Ventricular arrhythmia indication 44103008
Supraventricular arrhythmia indication 72654001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.75 acidic
pKa2 8.32 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
FE5SPV1Z6G UNII
D10503 KEGG_DRUG
57530-40-2 SECONDARY_CAS_RN
C0059688 UMLSCUI
CHEBI:134732 CHEBI
CHEMBL1997663 ChEMBL_ID
107841 PUBCHEM_CID
DB13645 DRUGBANK_ID
C046818 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None