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glafenine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| analgesics, glafenine derivatives (subgroup of fenamic acid group) | 1297 | 3820-67-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.80 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 0.02 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.085 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.127 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 38.905 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 58.345 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 8.150 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 18.330 | % | High | 1 |
| herg | hERG pIC50 | 5.971 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 74.302 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 94.624 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 5.350 | % | High | 1 |
| kinase-safety-class | ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CHEK1,CSF1R,CSK,DDR1,DYRK1B,EGFR,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT3,FYN,GAK,GRK2,GSK3B,IKBKB,INSR,IRAK1,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK14,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MINK1,MTOR,NTRK1,NTRK2,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,PTK6,RIPK3,SIK2,SIK3,SRC,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1 | 92 | |||
| kinase-selectivity-class | ACVR1B,ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKC,AXL,BRAF,CAMK2D,CDK9,DDR1,DYRK1B,EPHA2,EPHB4,ERBB2,FLT3,MAP3K21,MAP4K1,MAP4K3,MAPK7,MARK4,SIK2,SIK3,STK10,STK33,SYK,TGFBR1,TTK,ULK1 | 30 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 5.649 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 230.144 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 6.470 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 16.218 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 13.820 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 260.615 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 43.930 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 5.360 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 13.092 | uM | High | 1 |
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:
| Source | Code | Description |
|---|---|---|
| ATC | N02BG03 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Other analgesics and antipyretics |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| CHEBI has role | CHEBI:35222 | inhibitor |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
Related Drugs by ATC class:
N02BG Other analgesics and antipyretics 8 drugs
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 | 13.75 | acidic |
| pKa2 | 6.97 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Bile salt export pump | Transporter | IC50 | 4.65 | CHEMBL | |||||
| Bile salt export pump | Transporter | IC50 | 4.49 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01351 | KEGG_DRUG |
| C0017592 | UMLSCUI |
| CHEBI:31653 | CHEBI |
| CHEMBL146095 | ChEMBL_ID |
| DB08963 | DRUGBANK_ID |
| D005897 | MESH_DESCRIPTOR_UI |
| 3474 | PUBCHEM_CID |
| 1890 | INN_ID |
| 65513-72-6 | SECONDARY_CAS_RN |
| 46HL4I09AH | UNII |
| 006856 | NDDF |
Pharmaceutical products:
None