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fendiline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1148 | 13042-18-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Coronary vasodilator; inhibits calcium function in muscle cells in excitation-contraction coupling; proposed as antiarrhythmic and antianginal agents.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 9 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.415 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.570 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 14.028 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 21.380 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.950 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 3.990 | % | High | 1 |
| herg | hERG pIC50 | 6.108 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 13.772 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 54.200 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.320 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 50 | |||
| kinase-selectivity-class | AKT3,AXL,GRK2,PDK4,SIK2 | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.862 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 138.357 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.640 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.501 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 5.190 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 237.137 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 8.790 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.840 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 234.963 | 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 | C08EA01 | CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS NON-SELECTIVE CALCIUM CHANNEL BLOCKERS Phenylalkylamine derivatives |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ischemic heart disease | indication | 414545008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.97 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.49 | CHEMBL | |||||
| Extracellular calcium-sensing receptor | GPCR | EC50 | 6 | CHEMBL | |||||
| Sphingomyelin phosphodiesterase | Enzyme | IC50 | 5.25 | CHEMBL | |||||
| Transcriptional activator protein luxR | Transcription factor | IC50 | 4.04 | CHEMBL | |||||
| Calmodulin | Cytosolic other | Kd | 6.30 | CHEMBL | |||||
| Extracellular calcium-sensing receptor | GPCR | POSITIVE ALLOSTERIC MODULATOR | EC50 | 4.92 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| N0000166521 | NUI |
| D07185 | KEGG_DRUG |
| 13636-18-5 | SECONDARY_CAS_RN |
| C0015824 | UMLSCUI |
| CHEBI:748824 | CHEBI |
| CHEMBL254832 | ChEMBL_ID |
| CHEMBL1405922 | ChEMBL_ID |
| DB08980 | DRUGBANK_ID |
| D005275 | MESH_DESCRIPTOR_UI |
| 3336 | PUBCHEM_CID |
| 2924 | INN_ID |
| S253D559A8 | UNII |
| 236767 | RXNORM |
| 006773 | NDDF |
| 006774 | NDDF |
| S253D559A8 | INXIGHT DRUGS |
Pharmaceutical products:
None