ripasudil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Rho protein kinase inhibitors 4938 223645-67-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ripasudil
  • ripasudil hydrochloride hydrate
  • ripasudil hydrochloride
  • glanatec
  • glanatec ophthalmic solution
  • ripasudil HCl
Rho-associated kinase inhibitor for the treatment of glaucoma and ocular hypertension
  • Molecular weight: 323.39
  • Formula: C15H18FN3O2S
  • CLOGP: 1.73
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 62.30
  • ALOGS: -3.03
  • ROTB: 1

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 26, 2014 PMDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01EX07 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Other antiglaucoma preparations

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Glaucoma indication 23986001 DOID:1686

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.12 Basic
pKa2 4.91 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 IC50 7.29 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Rho-associated protein kinase 2 Kinase INHIBITOR IC50 7.72 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Serine/threonine-protein kinase MARK2 Kinase Kd 5.22 CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1 Kinase Kd 5.49 CHEMBL
Serine/threonine-protein kinase PLK4 Kinase Kd 5.09 CHEMBL
Serine/threonine-protein kinase N1 Kinase Kd 6.38 CHEMBL
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 4.24 CHEMBL
Cyclin-dependent kinase 9 Kinase Kd 4.88 CHEMBL
Serine/threonine-protein kinase N2 Kinase Kd 6.54 CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 5.43 CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha Kinase INHIBITOR IC50 5.68 IUPHAR
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 5.49 CHEMBL
Aurora kinase B Kinase Kd 5.94 CHEMBL
Serine/threonine-protein kinase D2 Kinase Kd 5.43 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 4.93 CHEMBL
5'-AMP-activated protein kinase subunit gamma-1 Kinase Kd 5.74 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3 Kinase Kd 5.51 CHEMBL
Protein kinase C delta type Kinase Kd 5.61 CHEMBL

External reference:

IDSource
D10463 KEGG_DRUG
CHEBI:136046 CHEBI
CHEMBL3426621 ChEMBL_ID
C584679 MESH_SUPPLEMENTAL_RECORD_UI
10423 IUPHAR_LIGAND_ID
9691 INN_ID
DB13165 DRUGBANK_ID
11978226XX UNII
9863672 PUBCHEM_CID
018524 NDDF
018525 NDDF
C4045501 UMLSCUI
CHEMBL4594454 ChEMBL_ID

Pharmaceutical products:

None