Assay Detail
Binding
CHEMBL2161920
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Inhibition of recombinant Plasmodium falciparum falcipain 2 incubated with compound for 10 mins before addition of Z-Phe-Arg-AMC substrate by fluorescence spectrophotometry
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.11 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374508 | E-64 | — | 1 | 7.70 |
| CHEMBL2158883 | — | — | 1 | 5.22 |
| CHEMBL2158886 | — | — | 1 | 5.16 |
| CHEMBL2158177 | — | — | 1 | 4.92 |
| CHEMBL2158881 | — | — | 1 | 4.85 |
| CHEMBL2158888 | — | — | 1 | 4.82 |
| CHEMBL2158879 | — | — | 1 | 4.80 |
| CHEMBL2158182 | — | — | 1 | 4.75 |
| CHEMBL2158175 | — | — | 1 | 4.72 |
| CHEMBL2158885 | — | — | 1 | 4.68 |
| CHEMBL2158887 | — | — | 1 | 4.64 |
| CHEMBL2158875 | — | — | 1 | - |
| CHEMBL2158183 | — | — | 1 | - |
| CHEMBL1424094 | — | — | 1 | - |
| CHEMBL2158181 | — | — | 1 | - |
| CHEMBL2158180 | — | — | 1 | - |
| CHEMBL2158179 | — | — | 1 | - |
| CHEMBL2158178 | — | — | 1 | - |
| CHEMBL2158176 | — | — | 1 | - |
| CHEMBL2158174 | — | — | 1 | - |
| CHEMBL2158889 | — | — | 1 | - |
| CHEMBL2158876 | — | — | 1 | - |
| CHEMBL2158877 | — | — | 1 | - |
| CHEMBL2158878 | — | — | 1 | - |
| CHEMBL2158884 | — | — | 1 | - |
| CHEMBL2158880 | — | — | 1 | - |
| CHEMBL2158882 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374508 | E-64 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2158883 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2158886 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2158177 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2158881 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2158888 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2158879 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2158182 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2158175 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2158885 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2158887 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2158875 | — | IC50 | - | — | - | |
| CHEMBL2158183 | — | IC50 | - | — | - | |
| CHEMBL1424094 | — | IC50 | - | — | - | |
| CHEMBL2158181 | — | IC50 | - | — | - | |
| CHEMBL2158180 | — | IC50 | - | — | - | |
| CHEMBL2158179 | — | IC50 | - | — | - | |
| CHEMBL2158178 | — | IC50 | - | — | - | |
| CHEMBL2158176 | — | IC50 | - | — | - | |
| CHEMBL2158174 | — | IC50 | - | — | - | |
| CHEMBL2158889 | — | IC50 | - | — | - | |
| CHEMBL2158876 | — | IC50 | - | — | - | |
| CHEMBL2158877 | — | IC50 | - | — | - | |
| CHEMBL2158878 | — | IC50 | - | — | - | |
| CHEMBL2158884 | — | IC50 | - | — | - | |
| CHEMBL2158880 | — | IC50 | - | — | - | |
| CHEMBL2158882 | — | IC50 | - | — | - |