Assay Detail
Binding
CHEMBL764688
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In vitro inhibition of aspartic protease plasmepsin-1 (Plm) of Plasmodium falciparum.
22
Total Activities
22
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 | 22 | 7.75 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112598 | — | — | 1 | 9.30 |
| CHEMBL113331 | — | — | 1 | 8.47 |
| CHEMBL112468 | — | — | 1 | 8.41 |
| CHEMBL443541 | — | — | 1 | 8.39 |
| CHEMBL114634 | — | — | 1 | 8.27 |
| CHEMBL325768 | — | — | 1 | 8.27 |
| CHEMBL324009 | — | — | 1 | 8.19 |
| CHEMBL325240 | — | — | 1 | 8.17 |
| CHEMBL114278 | — | — | 1 | 8.09 |
| CHEMBL115297 | — | — | 1 | 8.05 |
| CHEMBL113208 | — | — | 1 | 7.80 |
| CHEMBL112935 | — | — | 1 | 7.62 |
| CHEMBL115660 | — | — | 1 | 7.57 |
| CHEMBL113876 | — | — | 1 | 7.54 |
| CHEMBL112212 | — | — | 1 | 7.50 |
| CHEMBL115214 | — | — | 1 | 7.40 |
| CHEMBL324737 | — | — | 1 | 7.31 |
| CHEMBL116282 | — | — | 1 | 7.28 |
| CHEMBL112261 | — | — | 1 | 7.24 |
| CHEMBL116267 | — | — | 1 | 7.23 |
| CHEMBL322979 | — | — | 1 | 6.21 |
| CHEMBL111720 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112598 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL113331 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL112468 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL443541 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL114634 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL325768 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL324009 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL325240 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL114278 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL115297 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL113208 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL112935 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL115660 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL113876 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL112212 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL115214 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL324737 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL116282 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL112261 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL116267 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL322979 | — | Ki | = | 619.0 | nM | 6.21 |
| CHEMBL111720 | — | Ki | = | 822.0 | nM | 6.08 |