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

Stem definitionDrug idCAS RN
4655 90961-53-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • KC-8857
  • tedisamil
  • tedisamil sesquifumarate
  • Molecular weight: 288.48
  • Formula: C19H32N2
  • CLOGP: 3.32
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 6.48
  • ALOGS: -4.13
  • ROTB: 4

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.665 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.951 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 6.823 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 6.295 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 57.200 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 70.430 % High 1
herg hERG pIC50 4.704 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.258 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.715 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 32.830 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,IRAK4,ITK,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1 23
kinase-selectivity-class ACVRL1,AXL,CHUK,EIF2AK3,MAP2K6,PIK3CD 6
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.738 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.350 High 1
mh-clint Mouse hepatocyte intrinsic clearance 17.378 High 1
mppb Mouse plasma protein binding (% unbound) 53.220 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.766 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 69.070 % High 1
rat-kpuu-brain Rat brain Kpuu 1.315 % High 1
rh-clint Rat hepatocyte intrinsic clearance 107.647 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 28.010 % High 1
rppb Rat plasma protein binding (% unbound) 54.820 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 605.341 uM High 1

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 C01BD06 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
ANTIARRHYTHMICS, CLASS I AND III
Antiarrhythmics, class III
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D020011 Protective Agents
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:50509 potassium channel blocker

Related Drugs by ATC class:

C01BD Antiarrhythmics, class III 6 drugs
amiodaronebretyliumbunaftinedofetilidedronedaroneibutilide

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.69 Basic
pKa2 7.78 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 A member 7 Ion channel BLOCKER IC50 4.70 IUPHAR

External reference:

IDSource
D06652 KEGG_DRUG
CHEBI:134747 CHEBI
CHEMBL113461 ChEMBL_ID
CHEMBL2107378 ChEMBL_ID
C059921 MESH_SUPPLEMENTAL_RECORD_UI
2567 IUPHAR_LIGAND_ID
6297 INN_ID
150501-62-5 SECONDARY_CAS_RN
DB06200 DRUGBANK_ID
A5VAY2U3R8 UNII
713431000 SNOMEDCT_US
C0076034 UMLSCUI
65825 PUBCHEM_CID

Pharmaceutical products:

None