Assay Detail
Binding
CHEMBL3767016
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Inhibition of Plasmodium falciparum plasmepsin 2 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 | 9 — Direct single protein target |
| 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 | 5.67 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3764174 | — | — | 1 | 6.82 |
| CHEMBL3763261 | — | — | 1 | 6.64 |
| CHEMBL3763404 | — | — | 1 | 6.47 |
| CHEMBL3765358 | — | — | 1 | 6.40 |
| CHEMBL3764405 | — | — | 2 | 6.24 |
| CHEMBL3764738 | — | — | 1 | 6.22 |
| CHEMBL3764953 | — | — | 1 | 5.80 |
| CHEMBL3765238 | — | — | 1 | 5.70 |
| CHEMBL3763442 | — | — | 1 | 5.70 |
| CHEMBL3764744 | — | — | 1 | 5.64 |
| CHEMBL3763159 | — | — | 1 | 5.62 |
| CHEMBL3763955 | — | — | 1 | 5.60 |
| CHEMBL3765317 | — | — | 1 | 5.58 |
| CHEMBL3764837 | — | — | 1 | 5.54 |
| CHEMBL3763524 | — | — | 1 | 5.28 |
| CHEMBL3763523 | — | — | 1 | 5.00 |
| CHEMBL3764518 | — | — | 1 | 4.97 |
| CHEMBL3763900 | — | — | 1 | 4.92 |
| CHEMBL3765557 | — | — | 1 | 4.90 |
| CHEMBL3763489 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3764174 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3763261 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3763404 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3765358 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3764405 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3764738 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3764953 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3765238 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3763442 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3764744 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3763159 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3763955 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3765317 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3764837 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3764405 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3763524 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3763523 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3764518 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL3763900 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3765557 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL3763489 | — | IC50 | = | 32000.0 | nM | 4.50 |