Assay Detail
Binding
CHEMBL4181679
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Inhibition of Plasmodium falciparum FP2 using Z-Leu-Arg-AMC as substrate preincubated for 30 min followed by substrate addition measured after 30 mins by spectrofluorimetric method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cysteine protease falcipain-2 (CHEMBL5801) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum |
Publication
Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.07 | 5.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4211317 | — | — | 1 | 5.31 |
| CHEMBL4207961 | — | — | 1 | 5.29 |
| CHEMBL4218177 | — | — | 1 | 5.21 |
| CHEMBL4218788 | — | — | 1 | 5.17 |
| CHEMBL1939368 | — | — | 1 | 5.16 |
| CHEMBL4211543 | — | — | 1 | 5.13 |
| CHEMBL4203015 | — | — | 1 | 5.12 |
| CHEMBL4212687 | — | — | 1 | 5.11 |
| CHEMBL4209200 | — | — | 1 | 5.04 |
| CHEMBL4209486 | — | — | 1 | 5.00 |
| CHEMBL4213904 | — | — | 1 | 5.00 |
| CHEMBL1458713 | — | — | 1 | 4.24 |
| CHEMBL4210479 | — | — | 1 | - |
| CHEMBL4214368 | — | — | 1 | - |
| CHEMBL4202708 | — | — | 1 | - |
| CHEMBL4210735 | — | — | 1 | - |
| CHEMBL4207059 | — | — | 1 | - |
| CHEMBL4206536 | — | — | 1 | - |
| CHEMBL4213489 | — | — | 1 | - |
| CHEMBL4203128 | — | — | 1 | - |
| CHEMBL4216274 | — | — | 1 | - |
| CHEMBL4213293 | — | — | 1 | - |
| CHEMBL4209975 | — | — | 1 | - |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4211317 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4207961 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4218177 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4218788 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1939368 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4211543 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4203015 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4212687 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4209200 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL4209486 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4213904 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1458713 | — | IC50 | = | 57200.0 | nM | 4.24 |
| CHEMBL4210479 | — | IC50 | - | — | - | |
| CHEMBL4214368 | — | IC50 | - | — | - | |
| CHEMBL4202708 | — | IC50 | - | — | - | |
| CHEMBL4210735 | — | IC50 | - | — | - | |
| CHEMBL4207059 | — | IC50 | - | — | - | |
| CHEMBL4206536 | — | IC50 | - | — | - | |
| CHEMBL4213489 | — | IC50 | - | — | - | |
| CHEMBL4203128 | — | IC50 | - | — | - | |
| CHEMBL4216274 | — | IC50 | - | — | - | |
| CHEMBL4213293 | — | IC50 | - | — | - | |
| CHEMBL4209975 | — | IC50 | - | — | - | |
| CHEMBL36 | PYRIMETHAMINE | IC50 | - | — | - |