Assay Detail
Functional
CHEMBL4768941
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antimalarial activity against Plasmodium falciparum T9/94 RC17 harboring DHFR A16V/S108T 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 | 7.63 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1231612 | — | — | 1 | 9.68 |
| CHEMBL4780381 | — | — | 1 | 9.62 |
| CHEMBL4782529 | — | — | 1 | 9.55 |
| CHEMBL4780298 | — | — | 1 | 9.49 |
| CHEMBL129788 | — | — | 1 | 9.47 |
| CHEMBL4798754 | — | — | 1 | 9.28 |
| CHEMBL587606 | — | — | 1 | 9.24 |
| CHEMBL4800011 | — | — | 1 | 9.24 |
| CHEMBL4784036 | — | — | 1 | 9.23 |
| CHEMBL4798400 | — | — | 1 | 9.14 |
| CHEMBL4789322 | — | — | 1 | 8.74 |
| CHEMBL4795771 | — | — | 1 | 8.62 |
| CHEMBL4788495 | — | — | 1 | 8.51 |
| CHEMBL4793581 | — | — | 1 | 8.49 |
| CHEMBL4800362 | — | — | 1 | 8.49 |
| CHEMBL4778245 | — | — | 1 | 8.43 |
| CHEMBL4780256 | — | — | 1 | 8.16 |
| CHEMBL4784738 | — | — | 1 | 7.77 |
| CHEMBL4798412 | — | — | 1 | 7.75 |
| CHEMBL4799632 | — | — | 1 | 7.60 |
| CHEMBL4791022 | — | — | 1 | 7.40 |
| CHEMBL4783968 | — | — | 1 | 7.31 |
| CHEMBL4795829 | — | — | 1 | 6.54 |
| CHEMBL4784378 | — | — | 1 | 6.37 |
| CHEMBL4779476 | — | — | 1 | 5.66 |
| CHEMBL4789386 | — | — | 1 | 5.46 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 5.43 |
| CHEMBL4786084 | — | — | 1 | 5.42 |
| CHEMBL4781350 | — | — | 1 | 5.41 |
| CHEMBL4798973 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1231612 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL4780381 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4782529 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4780298 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL129788 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4798754 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL587606 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4800011 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4784036 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4798400 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4789322 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4795771 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4788495 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4793581 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4800362 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4778245 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4780256 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4784738 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4798412 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4799632 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4791022 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4783968 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4795829 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4784378 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4779476 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4789386 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL747 | CYCLOGUANIL | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4786084 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4781350 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4798973 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4791594 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4789860 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4786930 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL4796554 | — | IC50 | - | — | - | |
| CHEMBL4781827 | — | IC50 | - | — | - | |
| CHEMBL4777058 | — | IC50 | - | — | - | |
| CHEMBL4796933 | — | IC50 | - | — | - | |
| CHEMBL4781162 | — | IC50 | - | — | - | |
| CHEMBL528489 | — | IC50 | - | — | - | |
| CHEMBL4796828 | — | IC50 | - | — | - | |
| CHEMBL527468 | — | IC50 | - | — | - | |
| CHEMBL4793034 | — | IC50 | - | — | - | |
| CHEMBL4792035 | — | IC50 | - | — | - | |
| CHEMBL4781149 | — | IC50 | - | — | - | |
| CHEMBL4796443 | — | IC50 | - | — | - | |
| CHEMBL4799272 | — | IC50 | - | — | - | |
| CHEMBL4792349 | — | IC50 | - | — | - | |
| CHEMBL4797103 | — | IC50 | - | — | - | |
| CHEMBL4800635 | — | IC50 | - | — | - |