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tranilast 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiasthmatics or antiallergics, not acting primarily as antihistaminics anti-allergic or anti-inflammatory, not acting as anti-histaminics | 2714 | 53902-12-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis; structure
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.193 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 20.277 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 30.061 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 6.383 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.840 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.850 | % | High | 1 |
| herg | hERG pIC50 | 4.301 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.321 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.206 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.300 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT3,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 | 59 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,JAK1,MAP2K3,MAP2K6,MAP3K21,MAPK12,MAPK7,MAPK8,MTOR,PDK4,PIK3CB,PIK3CD,PRKDC,SIK2,STK33,TEK,TTK,ULK1 | 29 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 12.503 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 29.309 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.490 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.129 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 2.080 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 18.450 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 72.590 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.190 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 903.649 | 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 |
|---|---|---|
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D006401 | Hematologic Agents |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D010975 | Platelet Aggregation Inhibitors |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| MeSH PA | D018926 | Anti-Allergic Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35842 | antirheumatic drug |
| CHEBI has role | CHEBI:38215 | calcium channel blocker |
| CHEBI has role | CHEBI:49167 | anti-asthmatic drug |
| CHEBI has role | CHEBI:50857 | anti-allergic agent |
| CHEBI has role | CHEBI:62868 | hepatoprotective agent |
| CHEBI has role | CHEBI:72768 | aryl hydrocarbon receptor agonist |
| CHEBI has role | CHEBI:76595 | nephroprotective agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertrophic scar | indication | 19843006 | |
| Atopic dermatitis | indication | 24079001 | DOID:3310 |
| Keloid scar | indication | 33659008 | |
| Allergic rhinitis | indication | 61582004 | |
| Asthma | indication | 195967001 | DOID:2841 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.97 | acidic |
| pKa2 | 11.7 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Hematopoietic prostaglandin D synthase | Enzyme | IC50 | 4.94 | CHEMBL | |||||
| Transient receptor potential cation channel subfamily V member 2 | Ion channel | BLOCKER | IC50 | 5 | IUPHAR | ||||
| NACHT, LRR and PYD domains-containing protein 3 | Cytosolic other | IC50 | 4.60 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D02027 | KEGG_DRUG |
| C0146337 | UMLSCUI |
| CHEBI:77572 | CHEBI |
| CHEMBL415324 | ChEMBL_ID |
| DB07615 | DRUGBANK_ID |
| C012293 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5282230 | PUBCHEM_CID |
| 6326 | IUPHAR_LIGAND_ID |
| 5070 | INN_ID |
| HVF50SMY6E | UNII |
| 57330 | RXNORM |
| 009960 | NDDF |
| D27 | PDB_CHEM_ID |
| HVF50SMY6E | INXIGHT DRUGS |
Pharmaceutical products:
None