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

Stem definitionDrug idCAS RN
619 84-01-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • chlorproethazine
  • RP 4909
  • 2-Chloro-10-(3-diethylaminopropyl)phenothiazine
  • Molecular weight: 346.92
  • Formula: C19H23ClN2S
  • CLOGP: 6.56
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 0
  • TPSA: 6.48
  • ALOGS: -5.51
  • ROTB: 6

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.293 Moderate 0.65
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.656 Moderate 0.65
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 11.455 10^-6 cm/s Moderate 0.65
dh-clint Dog hepatocyte intrinsic clearance 60.674 uL/min/10^6 cells Moderate 0.65
dppb Dog plasma protein binding (% unbound) 1.340 % Moderate 0.65
fcs-ppb Fetal calf serum protein binding (% unbound) 6.120 % Moderate 0.65
herg hERG pIC50 6.291 pIC50 Moderate 0.65
hh-clint Human hepatocyte intrinsic clearance 17.498 uL/min/10^6 cells Moderate 0.65
hlm-clint Human liver microsomal intrinsic clearance 35.481 uL/min/mg protein Moderate 0.65
hppb Human plasma protein binding (% unbound) 1.570 % Moderate 0.65
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,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK 53
kinase-selectivity-class AXL,EIF2AK3,PDK4 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.655 Moderate 0.65
mh-clint Mouse hepatocyte intrinsic clearance 149.279 Moderate 0.65
mppb Mouse plasma protein binding (% unbound) 1.880 Moderate 0.65
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 3.733 Moderate 0.65
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 Moderate 0.77
pppb Pig plasma protein binding (% unbound) 7.600 % Moderate 0.65
rh-clint Rat hepatocyte intrinsic clearance 319.890 uL/min/10^6 cells Moderate 0.65
rh-fuinc Rat hepatocyte fraction unbound in incubation 6.510 % Moderate 0.65
rppb Rat plasma protein binding (% unbound) 2.060 % Moderate 0.65
solubility-dd Solubility at pH 7.4 in DMSO 469.894 uM Moderate 0.65

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 N05AA07 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Phenothiazines with aliphatic side-chain
MeSH PA D002491 Central Nervous System Agents
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018373 Peripheral Nervous System Agents
CHEBI has role CHEBI:35476 antipsychotic agent

Related Drugs by ATC class:

N05AA Phenothiazines with aliphatic side-chain 6 drugs
acepromazinechlorpromazinecyamemazinelevomepromazinepromazinetriflupromazine

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 9.33 Basic
pKa2 2.21 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 Ki 7.98 PDSP
D(3) dopamine receptor GPCR Ki 7.99 PDSP
D(4) dopamine receptor GPCR Ki 7.64 PDSP

External reference:

IDSource
D07308 KEGG_DRUG
59860 RXNORM
C0164858 UMLSCUI
CHEBI:135464 CHEBI
CHEMBL52125 ChEMBL_ID
DB13382 DRUGBANK_ID
C054028 MESH_SUPPLEMENTAL_RECORD_UI
65750 PUBCHEM_CID
1147 INN_ID
960NX27Z07 UNII
005317 NDDF

Pharmaceutical products:

None