Assay Detail
Binding
CHEMBL3384272
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Inhibition of Plasmodium falciparum M17 incubated for 10 mins before H-Leu-NHMec substrate addition by fluorescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Leucine aminopeptidase (CHEMBL1293313) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum 3D7 |
Publication
Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 9.98 | 10.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3359700 | — | — | 1 | 10.96 |
| CHEMBL3359698 | — | — | 1 | 10.92 |
| CHEMBL3359699 | — | — | 1 | 10.85 |
| CHEMBL3359691 | — | — | 1 | 10.80 |
| CHEMBL3359690 | — | — | 1 | 10.72 |
| CHEMBL3359693 | — | — | 1 | 10.55 |
| CHEMBL3359688 | — | — | 1 | 10.52 |
| CHEMBL3359697 | — | — | 1 | 10.46 |
| CHEMBL3359694 | — | — | 1 | 10.42 |
| CHEMBL3359692 | — | — | 1 | 10.28 |
| CHEMBL3359695 | — | — | 1 | 9.81 |
| CHEMBL3359689 | — | — | 1 | 7.07 |
| CHEMBL3359686 | — | — | 1 | 6.33 |
| CHEMBL3359696 | — | — | 1 | - |
| CHEMBL3359687 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3359700 | — | Ki | = | 0.011 | nM | 10.96 |
| CHEMBL3359698 | — | Ki | = | 0.012 | nM | 10.92 |
| CHEMBL3359699 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL3359691 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL3359690 | — | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL3359693 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL3359688 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3359697 | — | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL3359694 | — | Ki | = | 0.038 | nM | 10.42 |
| CHEMBL3359692 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL3359695 | — | Ki | = | 0.154 | nM | 9.81 |
| CHEMBL3359689 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL3359686 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL3359696 | — | Ki | = | 0.008 | nM | - |
| CHEMBL3359687 | — | Ki | > | 500.0 | nM | - |