Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL799

CILOSTAZOL
💊 Approved Drug
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
💊 Approved Drug
O=C1CCc2cc(OCCCCc3nnnn3C3CCCCC3)ccc2N1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL799
Name CILOSTAZOL
Phase Approved
Structure Type MOL
InChI Key RRGUKTPIGVIEKM-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

Cilostazol NSC-758936 OPC-13013 OPC-21 Pletal
11
Targets
28
Activities
1
Assay Types
0
PK Parameters
20
Publications
5
Known Names
20
Indications
1
Mechanisms

Molecular Properties

369.5
MW (Da)
3.46
ALogP
6
HBA
1
HBD
81.9
PSA (Ų)
0.76
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1999
Availability Prescription
Chirality Achiral

Routes of Administration

Oral

Flags

Black Box Warning Natural Product
USAN Year 1997

Extended Properties

Molecular Formula C20H27N5O2
MW 369.47
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.52

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Phosphodiesterase 3A inhibitor INHIBITOR cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A ✓ ✓

Indications

Thrombosis Arthritis, Rheumatoid Atherosclerosis Cardiovascular Diseases Cerebral Infarction Cerebrovascular Disorders Coronary Disease Ischemic Stroke Peripheral Arterial Disease Peripheral Vascular Diseases Cerebral Small Vessel Diseases Cognitive Dysfunction Heart Failure Intermittent Claudication Stroke Urticaria Wounds and Injuries CADASIL Fatty Liver Osteoarthritis

ATC Classification

B01AC23
cilostazol
Level 1: BLOOD AND BLOOD FORMING ORGANS
Level 2: ANTITHROMBOTIC AGENTS

Drug Warnings

Black Box Warning
General Warning
Country: United States

Activity Summary

IC50 28 meas. best 8.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
CHEMBL241
 IC50 8.41 7.99 3.9 2
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B
CHEMBL290
 IC50 7.3 7.3 50.0 1
Phosphodiesterase 3
CHEMBL2094125
 IC50 6.72 6.5125 190.0 4
Unchecked
CHEMBL612545
 IC50 6.7 6.242 200.0 5
Cytochrome P450 2C9
CHEMBL3397
 IC50 5.0 5.0 10000.0 1
Plasmodium falciparum
CHEMBL364
 IC50 5.0 4.96 10000.0 5
ATP-binding cassette sub-family C member 4
CHEMBL1743128
 IC50 4.78 4.78 16600.0 1
Oryctolagus cuniculus
CHEMBL374
 IC50 4.51 4.51 31000.0 1
NON-PROTEIN TARGET
CHEMBL3879801
 IC50 4.4 4.27 40000.0 2
Plasma
CHEMBL613652
 IC50 4.4 4.2433 40000.0 3
Voltage-gated L-type calcium channel
CHEMBL2095229
 IC50 4.04 4.04 91200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A IC50 = 3.89 nM 8.41 Inhibition of human PDE3A expressed in Sf9 cells using cAMP as substrate after 3... 32503691
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A IC50 = 27.0 nM 7.57 Inhibition of PDE3A (unknown origin) using FAM-cAMP as substrate incubated for 4... 38614063
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B IC50 = 50.0 nM 7.3 Inhibition of human recombinant PDE3B using FAM-cyclic-3',5'-AMP as substrate in... 38614063
Phosphodiesterase 3 IC50 = 190.0 nM 6.72 Inhibition of low Km cAMP phosphodiesterase PDE III of human platelets 2985781
Unchecked IC50 = 200.0 nM 6.7 Inhibition of PDE3 (unknown origin) 29363967
Unchecked IC50 = 200.0 nM 6.7 Inhibition of PDE3 (unknown origin) 29574203
Unchecked IC50 = 200.0 nM 6.7 Inhibition of PDE3 (unknown origin) 35144038
Phosphodiesterase 3 IC50 = 200.0 nM 6.7 Inhibition of human recombinant PDE3 expressed in Escherichia coli 37077378
Unchecked IC50 = 271.0 nM 6.57 DRUGMATRIX: Phosphodiesterase PDE3 enzyme inhibition (substrate: [3H]cAMP + cAMP... -
Phosphodiesterase 3 IC50 = 280.0 nM 6.55 Inhibition of human platelet PDE3 17500510
Phosphodiesterase 3 IC50 = 840.0 nM 6.08 Inhibition of human recombinant PDE3 catalytic domain expressed in baculovirus-i... 19303290
Plasmodium falciparum IC50 = 10000.0 nM 5.0 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910
Cytochrome P450 2C9 IC50 = 10000.0 nM 5.0 DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) -
Plasmodium falciparum IC50 = 10000.0 nM 5.0 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 10000.0 nM 5.0 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
ATP-binding cassette sub-family C member 4 IC50 = 16600.0 nM 4.78 Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as... 23956101
Unchecked IC50 = 29000.0 nM 4.54 In vitro inhibitory activity against Adenosine diphosphate (ADP) induced rabbit ... 9873372
Oryctolagus cuniculus IC50 = 31000.0 nM 4.51 In vitro inhibitory activity against collagen induced rabbit platelet aggregatio... 9873372

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885881 Rattus norvegicus 199
19734910 10.1038/nchembio.215 Plasmodium falciparum 5
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
37468498 10.1038/s41467-023-40064-9 Nuclear receptor subfamily 1 group I member 2 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 3
17500510 10.1021/jm0611511 Plasma 3
23425969 10.1016/j.ejmech.2013.01.026 NON-PROTEIN TARGET 3
37468498 10.1038/s41467-023-40064-9 Progesterone receptor 3
37468498 10.1038/s41467-023-40064-9 Androgen receptor 3
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 3
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 2
26948801 10.1016/j.drudis.2016.02.015 Homo sapiens 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
37468498 10.1038/s41467-023-40064-9 Voltage-dependent L-type calcium channel subunit alpha-1C 2
37468498 10.1038/s41467-023-40064-9 Mu-type opioid receptor 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
33640707 10.1016/j.bmc.2021.116074 Amyloid-beta precursor protein 2

Data from ChEMBL 36 via Core Engine