Assay Detail
Functional
CHEMBL763685
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Inhibition of hematin polymerization
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Histidine-rich protein PFHRP-II (CHEMBL1923) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum |
Publication
Structural specificity of chloroquine-hematin binding related to inhibition of hematin polymerization and parasite growth.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.58 | 4.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 4.82 |
| CHEMBL343728 | — | — | 1 | 4.82 |
| CHEMBL1236 | DESETHYLCHLOROQUINE | — | 1 | 4.82 |
| CHEMBL44789 | — | — | 1 | 4.80 |
| CHEMBL143042 | — | — | 1 | 4.77 |
| CHEMBL139984 | — | — | 1 | 4.75 |
| CHEMBL344599 | — | — | 1 | 4.75 |
| CHEMBL342499 | — | — | 1 | 4.52 |
| CHEMBL423184 | — | — | 1 | 4.22 |
| CHEMBL143439 | — | — | 1 | 4.16 |
| CHEMBL143522 | — | — | 1 | 4.00 |
| CHEMBL143177 | — | — | 1 | - |
| CHEMBL142884 | — | — | 1 | - |
| CHEMBL143331 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76 | CHLOROQUINE | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL343728 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1236 | DESETHYLCHLOROQUINE | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL44789 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL143042 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL139984 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL344599 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL342499 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL423184 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL143439 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL143522 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL143177 | — | IC50 | > | 2500000.0 | nM | - |
| CHEMBL142884 | — | IC50 | > | 2500000.0 | nM | - |
| CHEMBL143331 | — | IC50 | > | 2500000.0 | nM | - |