Assay Detail
Binding
CHEMBL764693
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In vitro inhibition of aspartic protease plasmepsin (Plm) II of Plasmodium falciparum
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.33 | 9.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113208 | — | — | 1 | 9.25 |
| CHEMBL112598 | — | — | 1 | 8.66 |
| CHEMBL33989 | — | — | 1 | 8.37 |
| CHEMBL113331 | — | — | 1 | 8.00 |
| CHEMBL325768 | — | — | 1 | 7.96 |
| CHEMBL324009 | — | — | 1 | 7.82 |
| CHEMBL443541 | — | — | 1 | 7.60 |
| CHEMBL325240 | — | — | 1 | 7.54 |
| CHEMBL114634 | — | — | 1 | 7.52 |
| CHEMBL112468 | — | — | 1 | 7.39 |
| CHEMBL115660 | — | — | 1 | 7.34 |
| CHEMBL114278 | — | — | 1 | 7.17 |
| CHEMBL115297 | — | — | 1 | 7.13 |
| CHEMBL112212 | — | — | 1 | 7.04 |
| CHEMBL113876 | — | — | 1 | 6.88 |
| CHEMBL112261 | — | — | 1 | 6.86 |
| CHEMBL116267 | — | — | 1 | 6.84 |
| CHEMBL111720 | — | — | 1 | 6.64 |
| CHEMBL324737 | — | — | 1 | 6.61 |
| CHEMBL116282 | — | — | 1 | 6.59 |
| CHEMBL115214 | — | — | 1 | 6.55 |
| CHEMBL112935 | — | — | 1 | 6.46 |
| CHEMBL322979 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113208 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL112598 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL33989 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL113331 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL325768 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL324009 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL443541 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL325240 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL114634 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL112468 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL115660 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL114278 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL115297 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL112212 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL113876 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL112261 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL116267 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL111720 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL324737 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL116282 | — | Ki | = | 256.0 | nM | 6.59 |
| CHEMBL115214 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL112935 | — | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL322979 | — | Ki | = | 390.0 | nM | 6.41 |