AI ASSISTANT
Ask DrugCentral
Explore drug information in your own words.
Type a question in the search bar above to get started. Each question is answered independently.
Try a sample question
Select a question to fill the search bar, then submit it or edit it first.
AI can make mistakes. Verify answers against the original sources before relying on them.
sivelestat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| elastase inhibitors | 2452 | 127373-66-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
inhibitor of neutrophil elastase; structure given in first source
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.106 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 17.620 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 4.009 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 7.816 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.970 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 7.230 | % | High | 1 |
| herg | hERG pIC50 | 4.336 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 92.045 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 125.026 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.560 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K21,MAP3K7,MAPK1,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 | 57 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,DDR1,DYRK1B,EPHB4,GRK2,MAP2K6,MAPK7,PIK3CD,PRKDC,STK33,TEK | 13 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.256 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 77.446 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 3.940 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.069 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 2.180 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 125.603 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 71.810 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 2.280 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 950.605 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | PMDA |
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 |
|---|---|---|
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D011480 | Protease Inhibitors |
| MeSH PA | D015842 | Serine Proteinase Inhibitors |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute lung injury | indication | 315345002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.84 | acidic |
| pKa2 | 7.84 | acidic |
| pKa3 | 13.07 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Neutrophil elastase | Enzyme | Ki | 6.70 | CHEMBL | IUPHAR | ||||
| Prolyl endopeptidase FAP | Enzyme | Ki | 6.23 | CHEMBL | |||||
| Myeloblastin | Enzyme | IC50 | 6.47 | CHEMBL | |||||
| Neutrophil elastase | Enzyme | IC50 | 6.84 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D03788 | KEGG_DRUG |
| 201677-61-4 | SECONDARY_CAS_RN |
| C0130137 | UMLSCUI |
| CHEBI:135704 | CHEBI |
| CHEMBL76688 | ChEMBL_ID |
| CHEMBL3182314 | ChEMBL_ID |
| DB12863 | DRUGBANK_ID |
| C069195 | MESH_SUPPLEMENTAL_RECORD_UI |
| 6441 | IUPHAR_LIGAND_ID |
| 7703 | INN_ID |
| DWI62G0P59 | UNII |
| 107706 | PUBCHEM_CID |
| DWI62G0P59 | INXIGHT DRUGS |
Pharmaceutical products:
None