Compound Detail
CHEMBL1174
EPTIFIBATIDE 💊 Approved Drug
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💊 Approved Drug
N=C(N)NCCCC[C@@H]1NC(=O)CCSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O
Basic Information
| ChEMBL ID | CHEMBL1174 |
| Name | EPTIFIBATIDE |
| Phase | Approved |
| Structure Type | BOTH |
| InChI Key | CZKPOZZJODAYPZ-LROMGURASA-N |
| Therapeutic | ✓ Yes |
3
Targets
4
Activities
2
Assay Types
4
PK Parameters
20
Publications
5
Known Names
15
Indications
1
Mechanisms
Molecular Properties
832.0
MW (Da)
-1.84
ALogP
11
HBA
11
HBD
323.9
PSA (Ų)
0.05
QED
3
Ro5 Violations
10
Rot. Bonds
Drug Information
| Molecule Type | Protein |
| First Approval | 1998 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Integrin alpha-IIb/beta-3 inhibitor | INHIBITOR | Integrin alpha-IIb/beta-3 | ✓ | ✓ |
Indications
Acute Coronary Syndrome Angina, Unstable Myocardial Infarction Myocardial Infarction Thrombosis Cardiovascular Diseases Ischemic Stroke Myocardial Ischemia Brain Infarction Coronary Disease Pneumonia Shock, Septic ST Elevation Myocardial Infarction Stroke Anemia, Sickle Cell
ATC Classification
B01AC16
eptifibatide
Level 1: BLOOD AND BLOOD FORMING ORGANS
Level 2: ANTITHROMBOTIC AGENTS
Activity Summary
IC50 3 meas. best 7.92
Kd 1 meas. best 6.92
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 7.92 | 7.92 | 12.0 | 1 |
| Integrin alpha-V/beta-3 CHEMBL1907598 | Kd | 6.92 | 6.92 | 120.0 | 1 |
| Integrin alpha-IIb/beta-3 CHEMBL2093869 | IC50 | 6.85 | 6.545 | 140.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 1.2 | mL.min-1.kg-1 | Homo sapiens |
| Fu | 0.75 | - | Homo sapiens |
| MRT | 2.4 | hr | Homo sapiens |
| T1/2 | 4.2 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| NON-PROTEIN TARGET | IC50 | = | 12.0 | nM | 7.92 | Antiplatelet activity in platelet (unknown origin) assessed as inhibition of pla... | 24461295 |
| Integrin alpha-V/beta-3 | Kd | = | 120.0 | nM | 6.92 | Inhibition of human integrin alphavbeta3 (unknown origin) | 31999923 |
| Integrin alpha-IIb/beta-3 | IC50 | = | 140.0 | nM | 6.85 | Inhibition of human platelet aggregation collected with sodium citrate as antico... | 10999999 |
| Integrin alpha-IIb/beta-3 | IC50 | = | 570.0 | nM | 6.24 | Inhibition of fibrinogen binding to alpha IIb beta-3 integrin using thrombin inh... | 10999999 |
Literature References
Data from ChEMBL 36 via Core Engine