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efonidipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium channel blockers, nifedipine derivatives | 992 | 111011-63-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.368 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.924 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 6.561 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 46.452 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.210 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.410 | % | High | 1 |
| herg | hERG pIC50 | 4.947 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 130.317 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 276.058 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.340 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ZAP70 | 46 | |||
| kinase-selectivity-class | AXL,BRAF,GRK2,MAP2K6,STK33,TEK | 6 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.234 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 167.109 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.190 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 13.335 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.400 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 220.800 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 1.460 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.210 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 1.167 | 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 | D000959 | Antihypertensive Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004232 | Diuretics |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:38215 | calcium channel blocker |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.96 | Basic |
| pKa2 | 2.26 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Voltage-gated L-type calcium channel | Ion channel | BLOCKER | DRUG LABEL | SCIENTIFIC LITERATURE | |||||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | BLOCKER | IC50 | 6.62 | SCIENTIFIC LITERATURE | ||||
| Voltage-dependent T-type calcium channel subunit alpha-1G | Ion channel | BLOCKER | IC50 | 7 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| D07886 | KEGG_DRUG |
| C0286819 | UMLSCUI |
| CHEBI:135859 | CHEBI |
| CHEMBL2074922 | ChEMBL_ID |
| DB09235 | DRUGBANK_ID |
| C066425 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12565 | IUPHAR_LIGAND_ID |
| 6852 | INN_ID |
| 111011-53-1 | SECONDARY_CAS_RN |
| 40ZTP2T37Q | UNII |
| 119171 | PUBCHEM_CID |
| 010907 | NDDF |
| 010908 | NDDF |
Pharmaceutical products:
None