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ripasudil 🐶 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 | 4938 | 223645-67-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Rho-associated kinase inhibitor for the treatment of glaucoma and ocular hypertension
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT1,AKT2,AKT3,ALK,AURKB,AURKC,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK2,CDK5,CDK7,CDK9,CHEK1,CLK2,CLK4,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK1,GRK2,GSK3A,GSK3B,IRAK1,ITK,JAK1,KIT,MAP2K6,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CD,PRKACA,PRKCD,PRKDC,ROCK1,ROCK2,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2 | 67 | |||
| kinase-selectivity-class | AXL,CDK9,MAPK1,PDK1,PRKACA,PRKCD,ROCK1,SIK2 | 8 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 26, 2014 | PMDA | Kowa Company, Ltd |
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 | S01EA55 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Sympathomimetics in glaucoma therapy |
| ATC | S01EX07 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Other antiglaucoma preparations |
Related Drugs by ATC class:
S01EA Sympathomimetics in glaucoma therapy 5 drugs
S01EX Other antiglaucoma preparations 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ocular hypertension | indication | 4210003 | DOID:9282 |
| Glaucoma | indication | 23986001 | DOID:1686 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.12 | Basic |
| pKa2 | 4.91 | 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 | 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:
| ID | Source |
|---|---|
| D10463 | KEGG_DRUG |
| CHEMBL3426621 | ChEMBL_ID |
| C584679 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10423 | IUPHAR_LIGAND_ID |
| 887375-67-9 | SECONDARY_CAS_RN |
| DB13165 | DRUGBANK_ID |
| 018524 | NDDF |
| 018525 | NDDF |
| 1340029007 | SNOMEDCT_US |
| 1340117000 | SNOMEDCT_US |
| 1340149000 | SNOMEDCT_US |
| C4045501 | UMLSCUI |
| CHEBI:136046 | CHEBI |
| CHEMBL4594454 | ChEMBL_ID |
| 9691 | INN_ID |
| 9863672 | PUBCHEM_CID |
| 11978226XX | UNII |
| 11978226XX | INXIGHT DRUGS |
Pharmaceutical products:
None