Compound Detail
CHEMBL976
PRAZIQUANTEL 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL976 |
| Name | PRAZIQUANTEL |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | FSVJFNAIGNNGKK-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
6
Targets
31
Activities
2
Assay Types
7
PK Parameters
20
Publications
13
Known Names
7
Indications
2
Mechanisms
Molecular Properties
312.4
MW (Da)
2.53
ALogP
2
HBA
0
HBD
40.6
PSA (Ų)
0.80
QED
0
Ro5 Violations
1
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1982 |
| Availability | Prescription |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Voltage-activated calcium channel beta 1 subunit blocker | BLOCKER | Voltage-activated calcium channel beta 1 subunit | ✓ | ✓ |
| Voltage-activated calcium channel beta 2 subunit blocker | BLOCKER | Voltage-activated calcium channel beta 2 subunit | ✓ | ✓ |
Indications
Helminthiasis Infections Opisthorchiasis Schistosomiasis Cysticercosis Schistosomiasis haematobia Schistosomiasis mansoni
ATC Classification
P02BA01
praziquantel
Level 1: ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
Level 2: ANTHELMINTICS
Activity Summary
EC50 21 meas. best 7.07
IC50 10 meas. best 7.11
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Schistosoma mansoni CHEMBL612893 | IC50 | 7.11 | 6.59 | 77.0 | 3 |
| Schistosoma haematobium CHEMBL4296598 | EC50 | 7.07 | 7.07 | 84.4 | 1 |
| Unchecked CHEMBL612545 | EC50 | 7.0 | 6.7033 | 100.0 | 3 |
| Schistosoma mansoni CHEMBL612893 | EC50 | 6.97 | 6.37 | 106.9 | 15 |
| Schistosoma japonicum CHEMBL612644 | EC50 | 6.79 | 6.79 | 161.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 5.0 | 4.95 | 10000.0 | 2 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.22 | 4.1333 | 60270.0 | 3 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 15739.22 | ng.hr.mL-1 | Homo sapiens |
| CL | 17.38 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 52.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 790.0 | mL.min-1.g-1 | Mus musculus |
| Cmax | 3200.92 | nM | Homo sapiens |
| T1/2 | 1.5 | hr | Homo sapiens |
| Tmax | 3.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine