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mofezolac 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory agents, ibufenac derivatives | 1829 | 78967-07-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Cyclooxygenase 1 inhibitor; ; RN from Toxlit
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.054 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.046 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 43.351 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.761 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.270 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 3.330 | % | High | 1 |
| herg | hERG pIC50 | 4.556 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.070 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.499 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.930 | % | High | 1 |
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,MAP2K6,MAPK7,MAPKAPK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK,TGFBR1 | 23 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,DYRK1B,EIF2AK3,ERBB2,GRK2,PDK4 | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.977 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 19.543 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 2.700 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.216 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.810 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 12.647 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.070 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.900 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 944.061 | 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 | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D016861 | Cyclooxygenase Inhibitors |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.86 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | IC50 | 6.36 | CHEMBL | |||||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 8.85 | CHEMBL | |||||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 8.85 | CHEMBL | |||||
| Prostaglandin G/H synthase 2 | Enzyme | IC50 | 6.36 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01718 | KEGG_DRUG |
| C0043597 | UMLSCUI |
| CHEBI:31860 | CHEBI |
| 63X | PDB_CHEM_ID |
| CHEMBL259972 | ChEMBL_ID |
| C054999 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4237 | PUBCHEM_CID |
| 6701 | INN_ID |
| RVJ0BV3H3Y | UNII |
| 11469 | RXNORM |
| 008241 | NDDF |
| RVJ0BV3H3Y | INXIGHT DRUGS |
Pharmaceutical products:
None