Assay Detail
Functional
CHEMBL4768943
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antimalarial activity against Plasmodium falciparum W2 harboring DHFR N51I/C59R/S108N mutant infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measured after 20 hrs by radioactivity method
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Cell Type | Erythrocyte |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 6.73 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4782529 | — | — | 1 | 9.62 |
| CHEMBL1231612 | — | — | 1 | 9.09 |
| CHEMBL4780381 | — | — | 1 | 8.68 |
| CHEMBL4798400 | — | — | 1 | 8.48 |
| CHEMBL129788 | — | — | 1 | 8.38 |
| CHEMBL4789322 | — | — | 1 | 8.27 |
| CHEMBL4784036 | — | — | 1 | 8.23 |
| CHEMBL4795771 | — | — | 1 | 8.09 |
| CHEMBL587606 | — | — | 1 | 8.00 |
| CHEMBL4796933 | — | — | 1 | 7.62 |
| CHEMBL4793581 | — | — | 1 | 7.62 |
| CHEMBL4799272 | — | — | 1 | 7.55 |
| CHEMBL4792035 | — | — | 1 | 7.48 |
| CHEMBL4780298 | — | — | 1 | 7.46 |
| CHEMBL4796554 | — | — | 1 | 7.41 |
| CHEMBL4781149 | — | — | 1 | 7.37 |
| CHEMBL4778245 | — | — | 1 | 7.36 |
| CHEMBL527468 | — | — | 1 | 7.34 |
| CHEMBL4781827 | — | — | 1 | 7.29 |
| CHEMBL4784738 | — | — | 1 | 7.24 |
| CHEMBL4800362 | — | — | 1 | 7.22 |
| CHEMBL4797103 | — | — | 1 | 7.16 |
| CHEMBL4800635 | — | — | 1 | 7.15 |
| CHEMBL4800011 | — | — | 1 | 7.00 |
| CHEMBL4781162 | — | — | 1 | 6.92 |
| CHEMBL4798754 | — | — | 1 | 6.89 |
| CHEMBL4792349 | — | — | 1 | 6.82 |
| CHEMBL4780256 | — | — | 1 | 6.72 |
| CHEMBL4791022 | — | — | 1 | 6.64 |
| CHEMBL528489 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4782529 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL1231612 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL4780381 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4798400 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL129788 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4789322 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4784036 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4795771 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL587606 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4796933 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4793581 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4799272 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4792035 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4780298 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4796554 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4781149 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4778245 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL527468 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4781827 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4784738 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4800362 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4797103 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4800635 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4800011 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4781162 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4798754 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4792349 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4780256 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4791022 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL528489 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4793034 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4799632 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4783968 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4795829 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4798412 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4784378 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4796443 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL4777058 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4789386 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4798973 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4796828 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL747 | CYCLOGUANIL | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL4786084 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4791594 | — | IC50 | = | 13900.0 | nM | 4.86 |
| CHEMBL4779476 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL4781350 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL4788495 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL4786930 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL4789860 | — | IC50 | = | 26000.0 | nM | 4.58 |