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cycloguanil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 754 | 516-21-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
the active metabolite of proguanil; antifolate drug
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPK9,MARK4,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 51 | |||
| kinase-selectivity-class | ACVR2B,AXL,GRK2,MAPK7 | 4 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
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 | P01BB02 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Biguanides |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000962 | Antimalarials |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D005493 | Folic Acid Antagonists |
| CHEBI has role | CHEBI:38068 | antimalarial |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:35442 | antiparasitic agent |
| CHEBI has role | CHEBI:35820 | antiprotozoal drug |
| CHEBI has role | CHEBI:50683 | EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| CHEBI has role | CHEBI:73913 | antifolate |
Related Drugs by ATC class:
P01BB Biguanides 3 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 | 11.2 | Basic |
| pKa2 | 4.66 | Basic |
| pKa3 | 3.37 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Dihydrofolate reductase | Enzyme | Ki | 7.25 | CHEMBL | |||||
| Bifunctional dihydrofolate reductase-thymidylate synthase | Enzyme | INHIBITOR | Ki | 8.96 | CHEMBL | CHEMBL | |||
| Dihydrofolate reductase | Enzyme | Ki | 7.63 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | IC50 | 6.96 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | Ki | 5.99 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | Ki | 4.76 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | Ki | 6.95 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | Ki | 5.99 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 26RM326WVN | UNII |
| D02387 | KEGG_DRUG |
| 609-78-9 | SECONDARY_CAS_RN |
| C0056751 | UMLSCUI |
| 1CY | PDB_CHEM_ID |
| CHEMBL747 | ChEMBL_ID |
| 9049 | PUBCHEM_CID |
| DB14763 | DRUGBANK_ID |
| CHEMBL3989825 | ChEMBL_ID |
| C026009 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10027 | IUPHAR_LIGAND_ID |
| C073266 | MESH_SUPPLEMENTAL_RECORD_UI |
| 002945 | NDDF |
| 002946 | NDDF |
| 28223003 | SNOMEDCT_US |
| CHEBI:4003 | CHEBI |
| 1527 | INN_ID |
Pharmaceutical products:
None