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fasudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Rho protein kinase inhibitors | 1132 | 103745-39-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
intracellular calcium antagonist
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 1.22 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 77.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.44 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 20 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.170 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.432 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 2.831 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 8.017 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 68.130 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 76.230 | % | High | 1 |
| herg | hERG pIC50 | 4.516 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 13.243 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 14.158 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 63.740 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKB,AURKC,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK2,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK1,GRK2,GSK3B,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K10,MAP3K21,MAP3K7,MAPK1,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKACA,PRKCD,PRKDC,ROCK1,ROCK2,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2 | 64 | |||
| kinase-selectivity-class | AXL,BRAF,CAMK2D,CDK9,DYRK1B,EGFR,ERBB2,GRK2,JAK1,MAP3K21,MAPK1,MAPK7,MARK4,PRKACA,PRKCD,ROCK1,SIK2,SIK3,STK33,ULK1 | 20 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.460 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 427.563 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 76.760 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 4.498 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 71.530 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 101.859 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 94.650 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 65.940 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 970.510 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 30, 1995 | PMDA |
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 | C04AX32 | CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Other peripheral vasodilators |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D047428 | Protein Kinase Inhibitors |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:38215 | calcium channel blocker |
| CHEBI has role | CHEBI:48407 | antiparkinson drug |
| CHEBI has role | CHEBI:50925 | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor |
| CHEBI has role | CHEBI:63726 | neuroprotective agent |
| CHEBI has role | CHEBI:66980 | nootropic agent |
| CHEBI has role | CHEBI:176497 | geroprotector |
Related Drugs by ATC class:
C04AX Other peripheral vasodilators 16 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Spasm of cerebral arteries | indication | 73173006 | |
| Cerebral ischemia | indication | 287731003 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.04 | Basic |
| pKa2 | 5.74 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Rho-associated protein kinase 1 | Kinase | INHIBITOR | Ki | 7 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Rho-associated protein kinase 2 | Kinase | INHIBITOR | Kd | 7.11 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Myosin light chain kinase, smooth muscle | Kinase | Ki | 4.44 | CHEMBL | |||||
| Protein kinase C delta type | Kinase | Kd | 5.32 | CHEMBL | |||||
| Protein kinase C epsilon type | Kinase | IC50 | 5.52 | CHEMBL | |||||
| Serine/threonine-protein kinase N1 | Kinase | IC50 | 5.77 | CHEMBL | |||||
| BMP-2-inducible protein kinase | Kinase | Kd | 4.47 | CHEMBL | |||||
| Dual specificity protein kinase CLK1 | Kinase | Kd | 6.82 | CHEMBL | |||||
| Ribosomal protein S6 kinase alpha-5 | Kinase | IC50 | 5.30 | CHEMBL | |||||
| C-C motif chemokine 2 | Cytokine | IC50 | 5.16 | CHEMBL | |||||
| Cyclin-dependent kinase 9 | Kinase | Kd | 5.37 | CHEMBL | |||||
| Serine/threonine-protein kinase N2 | Kinase | IC50 | 6.11 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | Ki | 4.60 | CHEMBL | |||||
| Serine/threonine-protein kinase LATS1 | Kinase | Kd | 5.38 | CHEMBL | |||||
| cAMP-dependent protein kinase catalytic subunit alpha | Kinase | AC50 | 5.81 | CHEMBL | |||||
| Citron Rho-interacting kinase | Kinase | Kd | 4.31 | CHEMBL | |||||
| Serine/threonine-protein kinase D2 | Kinase | Kd | 5.19 | CHEMBL | |||||
| Serine/threonine-protein kinase D3 | Kinase | Kd | 4.63 | CHEMBL | |||||
| Cyclin-dependent kinase 13 | Kinase | Kd | 5.34 | CHEMBL | |||||
| Serine/threonine-protein kinase N3 | Kinase | Kd | 7 | CHEMBL | |||||
| Cyclin-dependent kinase 12 | Kinase | Kd | 5.46 | CHEMBL | |||||
| Maternal embryonic leucine zipper kinase | Kinase | Kd | 5.72 | CHEMBL | |||||
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Enzyme | Kd | 5.61 | CHEMBL | |||||
| Rho-associated protein kinase 2 | Kinase | IC50 | 5.72 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01840 | KEGG_DRUG |
| 105628-07-7 | SECONDARY_CAS_RN |
| C0062068 | UMLSCUI |
| CHEBI:43871 | CHEBI |
| M77 | PDB_CHEM_ID |
| CHEMBL38380 | ChEMBL_ID |
| CHEMBL541388 | ChEMBL_ID |
| DB08162 | DRUGBANK_ID |
| C049347 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3547 | PUBCHEM_CID |
| 5181 | IUPHAR_LIGAND_ID |
| 6696 | INN_ID |
| Q0CH43PGXS | UNII |
Pharmaceutical products:
None