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thiamphenicol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2624 | 15318-45-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A methylsulfonyl analog of CHLORAMPHENICOL. It is an antibiotic and immunosuppressive agent.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | O |
| 1.50 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 120.31 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.074 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 5.754 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.743 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.459 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 84.600 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 90.540 | % | High | 1 |
| herg | hERG pIC50 | 3.750 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.334 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.140 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 85.110 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK3,MAP2K6,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,STK33,SYK,TEK,TGFBR1,ZAP70 | 33 | |||
| kinase-selectivity-class | MAP2K6,PDK1,PDK2 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.422 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.957 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 87.240 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.639 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 85.650 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.406 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 97.240 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 80.970 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 920.450 | 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 | J01BA02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE AMPHENICOLS Amphenicols |
| ATC | J01BA52 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE AMPHENICOLS Amphenicols |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| CHEBI has role | CHEBI:33281 | antimicrobial agent |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
Related Drugs by ATC class:
J01BA Amphenicols 1 drug
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 | 9.75 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 2C19 | Enzyme | IC50 | 5.12 | WOMBAT-PK | |||||
| 50S ribosomal protein L10 | Ribosomal protein | WOMBAT-PK | |||||||
| Streptokinase A | Enzyme | EC50 | 5.77 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| N0000166816 | NUI |
| D01407 | KEGG_DRUG |
| C0039854 | UMLSCUI |
| CHEBI:32215 | CHEBI |
| TH8 | PDB_CHEM_ID |
| CHEMBL1236282 | ChEMBL_ID |
| DB08621 | DRUGBANK_ID |
| D013839 | MESH_DESCRIPTOR_UI |
| 27200 | PUBCHEM_CID |
| 12400 | IUPHAR_LIGAND_ID |
| 935 | INN_ID |
| FLQ7571NPM | UNII |
| 10463 | RXNORM |
| 005347 | NDDF |
| 363552000 | SNOMEDCT_US |
| 713763007 | SNOMEDCT_US |
Pharmaceutical products:
None