fasudil Indications/Contra | FAERs | Orange Book | 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

Approvals:

DateAgencyCompanyOrphan
June 30, 1995 PMDA

FDA Adverse Event Reporting System

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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Spasm of cerebral arteries indication 73173006
Cerebral ischemia indication 287731003

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
Ribosomal protein S6 kinase alpha-5 Kinase IC50 5.30 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Ki 4.44 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 N1 Kinase IC50 5.77 CHEMBL
C-C motif chemokine 2 Cytokine IC50 5.16 CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha Kinase AC50 5.81 CHEMBL
Protein kinase C epsilon type Kinase IC50 5.52 CHEMBL
Rho-associated protein kinase 2 Kinase IC50 5.72 CHEMBL

External reference:

IDSource
D01840 KEGG_DRUG
CHEBI:31593 CHEBI
CHEMBL38380 ChEMBL_ID
CHEMBL541388 ChEMBL_ID
Q0CH43PGXS UNII
6696 INN_ID
105628-07-7 SECONDARY_CAS_RN
M77 PDB_CHEM_ID
DB08162 DRUGBANK_ID
3547 PUBCHEM_CID
5181 IUPHAR_LIGAND_ID
C049347 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None