Assay Detail
Binding
CHEMBL3767015
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Inhibition of Plasmodium falciparum plasmepsin 4 preincubated for 30 mins followed by DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS substrate addition by FRET assay
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.10 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3764174 | — | — | 1 | 7.00 |
| CHEMBL3763523 | — | — | 1 | 6.89 |
| CHEMBL3763261 | — | — | 1 | 6.70 |
| CHEMBL3765358 | — | — | 1 | 6.52 |
| CHEMBL3763489 | — | — | 1 | 6.40 |
| CHEMBL3765317 | — | — | 1 | 6.40 |
| CHEMBL3764738 | — | — | 1 | 6.40 |
| CHEMBL3763404 | — | — | 1 | 6.30 |
| CHEMBL3764405 | — | — | 2 | 6.22 |
| CHEMBL3763442 | — | — | 1 | 6.16 |
| CHEMBL3763159 | — | — | 1 | 6.10 |
| CHEMBL3765238 | — | — | 1 | 6.00 |
| CHEMBL3764837 | — | — | 1 | 5.96 |
| CHEMBL3764518 | — | — | 1 | 5.92 |
| CHEMBL3763955 | — | — | 1 | 5.89 |
| CHEMBL3764744 | — | — | 1 | 5.89 |
| CHEMBL3764953 | — | — | 1 | 5.82 |
| CHEMBL3763900 | — | — | 1 | 5.70 |
| CHEMBL3763524 | — | — | 1 | 5.52 |
| CHEMBL3765557 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3764174 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3763523 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3763261 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3765358 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3763489 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3765317 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3764738 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3763404 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3764405 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3763442 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3763159 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3765238 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3764837 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3764518 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3763955 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3764744 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3764953 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3763900 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3764405 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3763524 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3765557 | — | IC50 | = | 20000.0 | nM | 4.70 |