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

Stem definitionDrug idCAS RN
516 2622-30-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • carphenazine
  • carfenazine
  • carphenazin
  • proketazine
  • carphenazine maleate
  • proketazine maleate
  • Molecular weight: 425.59
  • Formula: C24H31N3O2S
  • CLOGP: 3.44
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 47.02
  • ALOGS: -4.06
  • ROTB: 8
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.970 Moderate 0.69
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.012 Moderate 0.69
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 26.242 10^-6 cm/s Moderate 0.69
dh-clint Dog hepatocyte intrinsic clearance 48.753 uL/min/10^6 cells Moderate 0.69
dppb Dog plasma protein binding (% unbound) 5.670 % Moderate 0.69
fcs-ppb Fetal calf serum protein binding (% unbound) 13.650 % Moderate 0.69
herg hERG pIC50 5.740 pIC50 Moderate 0.69
hh-clint Human hepatocyte intrinsic clearance 38.548 uL/min/10^6 cells Moderate 0.69
hlm-clint Human liver microsomal intrinsic clearance 80.724 uL/min/mg protein Moderate 0.69
hppb Human plasma protein binding (% unbound) 4.570 % Moderate 0.69
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,INSR,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK 55
kinase-selectivity-class AXL,CDK4,EPHB4,PDK4,SIK2,STK33 6
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.436 Moderate 0.69
mh-clint Mouse hepatocyte intrinsic clearance 192.752 Moderate 0.69
mppb Mouse plasma protein binding (% unbound) 5.830 Moderate 0.69
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 12.331 Moderate 0.69
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 17.950 % Moderate 0.69
rh-clint Rat hepatocyte intrinsic clearance 192.752 uL/min/10^6 cells Moderate 0.69
rh-fuinc Rat hepatocyte fraction unbound in incubation 38.740 % Moderate 0.69
rppb Rat plasma protein binding (% unbound) 5.130 % Moderate 0.69
solubility-dd Solubility at pH 7.4 in DMSO 142.889 uM Moderate 0.69

Approvals:

DateAgencyCompanyOrphan
None FDA WYETH AYERST

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:37930 phenothiazine antipsychotic drug
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:50919 antiemetic

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

DiseaseRelationSNOMED_IDDOID
Chronic schizophrenia indication 83746006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.21 Basic
pKa2 4.21 Basic
pKa3 1.58 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
D(2) dopamine receptor GPCR ANTAGONIST DRUGBANK CHEMBL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST CHEMBL CHEMBL

External reference:

IDSource
D02644 KEGG_DRUG
C0771221 UMLSCUI
CHEBI:51235 CHEBI
CHEMBL1201328 ChEMBL_ID
CHEMBL2358147 ChEMBL_ID
DB01038 DRUGBANK_ID
2975-34-0 SECONDARY_CAS_RN
18104 PUBCHEM_CID
123579002 SNOMEDCT_US
782144003 SNOMEDCT_US
7140 IUPHAR_LIGAND_ID
1179 INN_ID
CLY16Y8Z7E UNII
001486 NDDF
004593 NDDF
CLY16Y8Z7E INXIGHT DRUGS

Pharmaceutical products:

None