Assay Detail
Binding
CHEMBL4331651
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Inhibition of Plasmodium falciparum plasmepsin 1 using DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS as substrate preincubated for 30 mins followed by substrate addition and measured every min for 8 to 15 mins by FRET assay
10
Total Activities
10
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 |
Publication
Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.61 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449824 | — | — | 1 | 6.11 |
| CHEMBL4475791 | — | — | 1 | 6.10 |
| CHEMBL4449532 | — | — | 1 | 5.96 |
| CHEMBL4555241 | — | — | 1 | 5.75 |
| CHEMBL4515147 | — | — | 1 | 5.70 |
| CHEMBL4454293 | — | — | 1 | 5.60 |
| CHEMBL2334376 | — | — | 1 | 5.51 |
| CHEMBL4464784 | — | — | 1 | 5.25 |
| CHEMBL4515257 | — | — | 1 | 5.13 |
| CHEMBL4520253 | — | — | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449824 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4475791 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4449532 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4555241 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4515147 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4454293 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2334376 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4464784 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4515257 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4520253 | — | IC50 | = | 10300.0 | nM | 4.99 |