Assay Detail
Binding
CHEMBL3384271
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Inhibition of Plasmodium falciparum M1 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
Aminopeptidase N (CHEMBL4117) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum FcB1/Columbia |
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 | 8.04 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3359693 | — | — | 1 | 9.15 |
| CHEMBL3359688 | — | — | 1 | 9.10 |
| CHEMBL3359696 | — | — | 1 | 8.72 |
| CHEMBL3359697 | — | — | 1 | 8.40 |
| CHEMBL3359699 | — | — | 1 | 8.26 |
| CHEMBL3359700 | — | — | 1 | 8.13 |
| CHEMBL3359698 | — | — | 1 | 7.95 |
| CHEMBL3359692 | — | — | 1 | 7.91 |
| CHEMBL3359694 | — | — | 1 | 7.82 |
| CHEMBL3359695 | — | — | 1 | 7.64 |
| CHEMBL3359691 | — | — | 1 | 7.38 |
| CHEMBL3359689 | — | — | 1 | 7.13 |
| CHEMBL3359690 | — | — | 1 | 6.95 |
| CHEMBL3359687 | — | — | 1 | - |
| CHEMBL3359686 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3359693 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3359688 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3359696 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3359697 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3359699 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL3359700 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL3359698 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL3359692 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL3359694 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL3359695 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3359691 | — | Ki | = | 41.3 | nM | 7.38 |
| CHEMBL3359689 | — | Ki | = | 74.5 | nM | 7.13 |
| CHEMBL3359690 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL3359687 | — | Ki | > | 500.0 | nM | - |
| CHEMBL3359686 | — | Ki | > | 500.0 | nM | - |