Assay Detail
Binding
CHEMBL4224043
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Plasmodium falciparum 3D7 FLN (55 to 1193 residues) expressed in Escherichia coli BL21 using Dabcyl-HKRHSFRMRG-EDANS as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum 3D7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Falcilysin (CHEMBL4295876) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum (isolate 3D7) |
Publication
Development of piperazine-based hydroxamic acid inhibitors against falcilysin, an essential malarial protease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.94 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4225532 | — | — | 1 | 5.82 |
| CHEMBL4226440 | — | — | 1 | 5.30 |
| CHEMBL4228497 | — | — | 1 | 5.22 |
| CHEMBL4227329 | — | — | 1 | 5.16 |
| CHEMBL4227286 | — | — | 1 | 5.10 |
| CHEMBL4228556 | — | — | 1 | 5.10 |
| CHEMBL125598 | — | — | 1 | 5.00 |
| CHEMBL4227719 | — | — | 1 | 5.00 |
| CHEMBL4227787 | — | — | 1 | 4.89 |
| CHEMBL4224730 | — | — | 1 | 4.85 |
| CHEMBL4225559 | — | — | 1 | 4.80 |
| CHEMBL4225657 | — | — | 1 | 4.52 |
| CHEMBL4229016 | — | — | 1 | 4.51 |
| CHEMBL4225259 | — | — | 1 | 4.46 |
| CHEMBL4226498 | — | — | 1 | 4.40 |
| CHEMBL421644 | — | — | 1 | - |
| CHEMBL4228814 | — | — | 1 | - |
| CHEMBL4225711 | — | — | 1 | - |
| CHEMBL4225755 | — | — | 1 | - |
| CHEMBL4228238 | — | — | 1 | - |
| CHEMBL4226235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4225532 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4226440 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4228497 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4227329 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4227286 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4228556 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL125598 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4227719 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4227787 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4224730 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4225559 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4225657 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4229016 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4225259 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL4226498 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL421644 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4228814 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4225711 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4225755 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4228238 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4226235 | — | IC50 | > | 50000.0 | nM | - |