Assay Detail
Binding
CHEMBL5375522
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Activation of Schistosoma mansoni in TRPM binding site of PZQ expressed in HEK293 cells assessed as effect in cytosolic Ca2+ level measured for 250 sec by Fuuo-4 NW staining based FLIPR assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Schistosoma mansoni |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
The Anthelmintic Activity of Praziquantel Analogs Correlates with Structure-Activity Relationships at TRPM<sub>PZQ</sub> Orthologs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.55 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1235551 | PRAZIQUANTEL, (R)- | 3.0 | 1 | 6.55 |
| CHEMBL976 | PRAZIQUANTEL | 4.0 | 1 | 6.19 |
| CHEMBL397867 | — | — | 1 | 4.92 |
| CHEMBL3264245 | — | — | 1 | 4.55 |
| CHEMBL5437867 | — | — | 1 | - |
| CHEMBL5420262 | — | — | 1 | - |
| CHEMBL5421728 | — | — | 1 | - |
| CHEMBL5415853 | — | — | 1 | - |
| CHEMBL5420375 | — | — | 1 | - |
| CHEMBL5409440 | — | — | 1 | - |
| CHEMBL5415464 | — | — | 1 | - |
| CHEMBL5397472 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1235551 | PRAZIQUANTEL, (R)- | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL976 | PRAZIQUANTEL | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL397867 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3264245 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL5437867 | — | EC50 | - | — | - | |
| CHEMBL5420262 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5421728 | — | EC50 | - | — | - | |
| CHEMBL5415853 | — | EC50 | - | — | - | |
| CHEMBL5420375 | — | EC50 | - | — | - | |
| CHEMBL5409440 | — | EC50 | - | — | - | |
| CHEMBL5415464 | — | EC50 | - | — | - | |
| CHEMBL5397472 | — | EC50 | - | — | - |