Assay Detail
Binding
CHEMBL4842477
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Inhibition of recombinant Plasmodium falciparum falcipain-2 expressed in Escherichia coli M15 assessed as reduction in free AMC release using Z-FR-AMC as a substrate measured over 30 mins by fluorometric assay
20
Total Activities
20
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
Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.23 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4857262 | — | — | 1 | 5.47 |
| CHEMBL4850572 | — | — | 1 | 5.45 |
| CHEMBL4868442 | — | — | 1 | 5.42 |
| CHEMBL4869807 | — | — | 1 | 5.25 |
| CHEMBL4856045 | — | — | 1 | 5.23 |
| CHEMBL4857754 | — | — | 1 | 5.12 |
| CHEMBL4853187 | — | — | 1 | 5.03 |
| CHEMBL4871791 | — | — | 1 | 4.87 |
| CHEMBL4864385 | — | — | 1 | - |
| CHEMBL4861198 | — | — | 1 | - |
| CHEMBL307261 | ARTENIMOL | 3.0 | 1 | - |
| CHEMBL4859406 | — | — | 1 | - |
| CHEMBL4858403 | — | — | 1 | - |
| CHEMBL4854350 | — | — | 1 | - |
| CHEMBL4870974 | — | — | 1 | - |
| CHEMBL4863049 | — | — | 1 | - |
| CHEMBL4859035 | — | — | 1 | - |
| CHEMBL4870203 | — | — | 1 | - |
| CHEMBL4845812 | — | — | 1 | - |
| CHEMBL4860649 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4857262 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL4850572 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL4868442 | — | IC50 | = | 3780.0 | nM | 5.42 |
| CHEMBL4869807 | — | IC50 | = | 5620.0 | nM | 5.25 |
| CHEMBL4856045 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4857754 | — | IC50 | = | 7670.0 | nM | 5.12 |
| CHEMBL4853187 | — | IC50 | = | 9380.0 | nM | 5.03 |
| CHEMBL4871791 | — | IC50 | = | 13460.0 | nM | 4.87 |
| CHEMBL4864385 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4861198 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL307261 | ARTENIMOL | IC50 | > | 100000.0 | nM | - |
| CHEMBL4859406 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4858403 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4854350 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4870974 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4863049 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4859035 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4870203 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4845812 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4860649 | — | IC50 | > | 100000.0 | nM | - |