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probucol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2269 | 23288-49-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 27.64 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 5 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 | 61 | |||
| kinase-selectivity-class | AXL,BRAF,CSF1R,DDR1,EPHB4,GRK2,PDK4 | 7 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 1, 1977 | FDA |
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:
| Source | Code | Description |
|---|---|---|
| ATC | C10AX02 | CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN Other lipid modifying agents |
| MeSH PA | D000924 | Anticholesteremic Agents |
| MeSH PA | D000960 | Hypolipidemic Agents |
| MeSH PA | D000963 | Antimetabolites |
| MeSH PA | D000975 | Antioxidants |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D057847 | Lipid Regulating Agents |
| CHEBI has role | CHEBI:22586 | antioxidant |
| CHEBI has role | CHEBI:35472 | anti-inflammatory drug |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35679 | antilipemic drug |
| CHEBI has role | CHEBI:35821 | anticholesteremic drug |
Related Drugs by ATC class:
C10AX Other lipid modifying agents 15 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypercholesterolemia | indication | 13644009 | |
| Hyperlipidemia | indication | 55822004 | DOID:1168 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.32 | acidic |
| pKa2 | 11.92 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| ATP-binding cassette sub-family A member 1 | Transporter | INHIBITOR | CHEMBL | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.69 | WOMBAT-PK | |||||
| Arachidonate 15-lipoxygenase | Enzyme | IC50 | 4.85 | CHEMBL | |||||
| NAD-dependent protein deacylase sirtuin-5, mitochondrial | Enzyme | IC50 | 5.80 | CHEMBL | |||||
| Serine protease hepsin | Enzyme | IC50 | 6.37 | CHEMBL | |||||
| Trypsin | Enzyme | IC50 | 4.47 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018611 | VUID |
| N0000146924 | NUI |
| D00476 | KEGG_DRUG |
| 4018611 | VANDF |
| C0033215 | UMLSCUI |
| CHEBI:8427 | CHEBI |
| CHEMBL608 | ChEMBL_ID |
| D011341 | MESH_DESCRIPTOR_UI |
| DB01599 | DRUGBANK_ID |
| 7277 | IUPHAR_LIGAND_ID |
| 2928 | INN_ID |
| P3CTH044XJ | UNII |
| 4912 | PUBCHEM_CID |
| 203350 | RXNORM |
| 1235 | MMSL |
| 5357 | MMSL |
| d00353 | MMSL |
| 002054 | NDDF |
| 32474005 | SNOMEDCT_US |
| 387178009 | SNOMEDCT_US |
| P3CTH044XJ | INXIGHT DRUGS |
Pharmaceutical products:
None