fasudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Rho protein kinase inhibitors 1132 103745-39-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fasudil HCl semihydrate
  • fasudil hydrochloride
  • fasudil
  • HA-1077
  • fasudil hydrochloride hydrate
  • HA1077
  • fasudil HCl
intracellular calcium antagonist
  • Molecular weight: 291.37
  • Formula: C14H17N3O2S
  • CLOGP: 1.04
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 62.30
  • ALOGS: -2.74
  • ROTB: 1

Drug dosage:

None

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
ATC C04AX32 CARDIOVASCULAR SYSTEM
PERIPHERAL VASODILATORS
PERIPHERAL VASODILATORS
Other peripheral vasodilators
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D047428 Protein Kinase Inhibitors
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35620 vasodilator agents
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:38215 calcium channel blockers
CHEBI has role CHEBI:50925 serine/threonine protein kinase inhibitor
CHEBI has role CHEBI:63726 neuroprotective agents
CHEBI has role CHEBI:66980 intelligence enhancer
CHEBI has role CHEBI:176497 geroprotectors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 5.61 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Ki 4.44 CHEMBL
Protein kinase C delta type Kinase Kd 5.32 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
Protein kinase C epsilon type Kinase IC50 5.52 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
Potassium voltage-gated channel subfamily H member 2 Ion channel Ki 4.60 CHEMBL
Rho-associated protein kinase 2 Kinase IC50 5.72 CHEMBL

External reference:

IDSource
D01840 KEGG_DRUG
105628-07-7 SECONDARY_CAS_RN
C0062068 UMLSCUI
CHEBI:43871 CHEBI
M77 PDB_CHEM_ID
CHEMBL541388 ChEMBL_ID
CHEMBL38380 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