All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
Rho protein kinase inhibitors	1132	103745-39-7

Description:

Molecule	Description
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:

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

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	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|

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	Q13464	ROCK1_HUMAN	INHIBITOR	Ki	7		CHEMBL	SCIENTIFIC LITERATURE
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN	INHIBITOR	Kd	7.11		CHEMBL	SCIENTIFIC LITERATURE
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	5.61		CHEMBL
Myosin light chain kinase, smooth muscle	Kinase	Q15746	MYLK_HUMAN		Ki	4.44		CHEMBL
Protein kinase C delta type	Kinase	Q05655	KPCD_HUMAN		Kd	5.32		CHEMBL
Serine/threonine-protein kinase N1	Kinase	Q16512	PKN1_HUMAN		IC50	5.77		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	4.47		CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	6.82		CHEMBL
Ribosomal protein S6 kinase alpha-5	Kinase	O75582	KS6A5_HUMAN		IC50	5.30		CHEMBL
C-C motif chemokine 2	Cytokine	P13500	CCL2_HUMAN		IC50	5.16		CHEMBL
Cyclin-dependent kinase 9	Kinase	P50750	CDK9_HUMAN		Kd	5.37		CHEMBL
Serine/threonine-protein kinase N2	Kinase	Q16513	PKN2_HUMAN		IC50	6.11		CHEMBL
Protein kinase C epsilon type	Kinase	Q02156	KPCE_HUMAN		IC50	5.52		CHEMBL
Serine/threonine-protein kinase LATS1	Kinase	O95835	LATS1_HUMAN		Kd	5.38		CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha	Kinase	P17612	KAPCA_HUMAN		AC50	5.81		CHEMBL
Citron Rho-interacting kinase	Kinase	O14578	CTRO_HUMAN		Kd	4.31		CHEMBL
Serine/threonine-protein kinase D2	Kinase	Q9BZL6	KPCD2_HUMAN		Kd	5.19		CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	4.63		CHEMBL
Cyclin-dependent kinase 13	Kinase	Q14004	CDK13_HUMAN		Kd	5.34		CHEMBL
Serine/threonine-protein kinase N3	Kinase	Q6P5Z2	PKN3_HUMAN		Kd	7		CHEMBL
Cyclin-dependent kinase 12	Kinase	Q9NYV4	CDK12_HUMAN		Kd	5.46		CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	5.72		CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	4.60		CHEMBL
Rho-associated protein kinase 2	Kinase		ROCK2_RAT		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
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