Assay Detail
Binding
CHEMBL4223544
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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 measured every 1 min within 8 to 15 mins by FRET assay
21
Total Activities
21
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
2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.16 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296588 | PEPSTATIN | 2.0 | 1 | 9.05 |
| CHEMBL4225298 | — | — | 1 | 7.70 |
| CHEMBL4225824 | — | — | 1 | 7.30 |
| CHEMBL4225299 | — | — | 1 | 7.10 |
| CHEMBL4226087 | — | — | 1 | 7.05 |
| CHEMBL3764174 | — | — | 1 | 6.52 |
| CHEMBL4226891 | — | — | 1 | 6.22 |
| CHEMBL4228456 | — | — | 1 | 6.16 |
| CHEMBL4228072 | — | — | 1 | 6.13 |
| CHEMBL4229013 | — | — | 1 | 6.00 |
| CHEMBL4224896 | — | — | 1 | 6.00 |
| CHEMBL4225394 | — | — | 1 | 5.89 |
| CHEMBL4228633 | — | — | 1 | 5.70 |
| CHEMBL4227074 | — | — | 1 | 5.62 |
| CHEMBL4227924 | — | — | 1 | 5.52 |
| CHEMBL3763523 | — | — | 1 | 5.50 |
| CHEMBL4229080 | — | — | 1 | 5.47 |
| CHEMBL4225038 | — | — | 1 | 5.46 |
| CHEMBL4228400 | — | — | 1 | 5.30 |
| CHEMBL4225481 | — | — | 1 | 4.94 |
| CHEMBL4226144 | — | — | 1 | 4.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296588 | PEPSTATIN | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4225298 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4225824 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4225299 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4226087 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3764174 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4226891 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4228456 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4228072 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4229013 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4224896 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4225394 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4228633 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4227074 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4227924 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3763523 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4229080 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4225038 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4228400 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4225481 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL4226144 | — | IC50 | = | 16700.0 | nM | 4.78 |