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

Stem definitionDrug idCAS RN
antihypertensives, hydrazinephthalazine derivatives 4689 17692-43-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • picodralazine
  • picodralazine hydrochloride
  • picodralazine HCl
  • Molecular weight: 251.29
  • Formula: C14H13N5
  • CLOGP: 1.74
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 76.72
  • ALOGS: -3.38
  • ROTB: 3

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.681 Moderate 0.67
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.323 Moderate 0.67
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 7.161 10^-6 cm/s Moderate 0.67
dh-clint Dog hepatocyte intrinsic clearance 3.214 uL/min/10^6 cells Moderate 0.67
dppb Dog plasma protein binding (% unbound) 64.960 % Moderate 0.67
fcs-ppb Fetal calf serum protein binding (% unbound) 66.100 % Moderate 0.67
herg hERG pIC50 4.476 pIC50 Moderate 0.67
hh-clint Human hepatocyte intrinsic clearance 2.404 uL/min/10^6 cells Moderate 0.67
hlm-clint Human liver microsomal intrinsic clearance 3.639 uL/min/mg protein Moderate 0.67
hppb Human plasma protein binding (% unbound) 49.190 % Moderate 0.67
kinase-safety-class ACVR2A,ACVR2B,AKT3,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK1,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAPK1,MAPK12,MAPK7,MAPK9,MARK4,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 55
kinase-selectivity-class AXL,BRAF,CDK9,DDR1,ERBB2,FLT1,KDR,MAP2K6,MARK4,PIK3CD 10
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 5.212 Moderate 0.67
mh-clint Mouse hepatocyte intrinsic clearance 44.875 Moderate 0.67
mppb Mouse plasma protein binding (% unbound) 66.100 Moderate 0.67
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 8.337 Moderate 0.67
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 76.060 % Moderate 0.67
rh-clint Rat hepatocyte intrinsic clearance 16.032 uL/min/10^6 cells Moderate 0.67
rh-fuinc Rat hepatocyte fraction unbound in incubation 84.660 % Moderate 0.67
rppb Rat plasma protein binding (% unbound) 54.650 % Moderate 0.67
solubility-dd Solubility at pH 7.4 in DMSO 1000 uM Moderate 0.67

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 C02LG03 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
Hydrazinophthalazine derivatives and diuretics
ATC C02LG73 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
Hydrazinophthalazine derivatives and diuretics

Related Drugs by ATC class:

C02LG Hydrazinophthalazine derivatives and diuretics 2 drugs

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 7.5 Basic
pKa2 5.37 Basic
pKa3 3.65 Basic
pKa4 3.11 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
C1882375 UMLSCUI
CHEBI:136022 CHEBI
CHEMBL1968696 ChEMBL_ID
2405 INN_ID
O9D004V63I UNII
71890 PUBCHEM_CID

Pharmaceutical products:

None