Assay Detail
Functional
CHEMBL4410616
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Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum V1/S expressing Dihydrofolate reductase N51I/C59R/S108N/I164L mutant infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 18 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting method
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
6-Hydrophobic aromatic substituent pyrimethamine analogues as potential antimalarials for pyrimethamine-resistant Plasmodium falciparum.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.38 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4590684 | — | — | 1 | 6.37 |
| CHEMBL4461699 | — | — | 1 | 6.36 |
| CHEMBL4586252 | — | — | 1 | 6.27 |
| CHEMBL4447272 | — | — | 1 | 5.85 |
| CHEMBL4452609 | — | — | 1 | 5.57 |
| CHEMBL4462327 | — | — | 1 | 5.52 |
| CHEMBL4565928 | — | — | 1 | 5.47 |
| CHEMBL4546946 | — | — | 1 | 5.41 |
| CHEMBL4515405 | — | — | 1 | 5.36 |
| CHEMBL4459902 | — | — | 1 | 5.32 |
| CHEMBL4444614 | — | — | 1 | 5.28 |
| CHEMBL4456065 | — | — | 1 | 5.26 |
| CHEMBL4468791 | — | — | 1 | 5.21 |
| CHEMBL4557136 | — | — | 1 | 5.21 |
| CHEMBL4558959 | — | — | 1 | 5.16 |
| CHEMBL4467953 | — | — | 1 | 5.10 |
| CHEMBL4437388 | — | — | 1 | 5.04 |
| CHEMBL4526752 | — | — | 1 | 4.95 |
| CHEMBL4566524 | — | — | 1 | 4.94 |
| CHEMBL4553483 | — | — | 1 | 4.82 |
| CHEMBL4441455 | — | — | 1 | 4.51 |
| CHEMBL4459356 | — | — | 1 | - |
| CHEMBL4588852 | — | — | 1 | - |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | - |
| CHEMBL4542001 | — | — | 1 | - |
| CHEMBL22148 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4590684 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4461699 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4586252 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4447272 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL4452609 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL4462327 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4565928 | — | IC50 | = | 3420.0 | nM | 5.47 |
| CHEMBL4546946 | — | IC50 | = | 3910.0 | nM | 5.41 |
| CHEMBL4515405 | — | IC50 | = | 4370.0 | nM | 5.36 |
| CHEMBL4459902 | — | IC50 | = | 4810.0 | nM | 5.32 |
| CHEMBL4444614 | — | IC50 | = | 5240.0 | nM | 5.28 |
| CHEMBL4456065 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4468791 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4557136 | — | IC50 | = | 6150.0 | nM | 5.21 |
| CHEMBL4558959 | — | IC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL4467953 | — | IC50 | = | 7890.0 | nM | 5.10 |
| CHEMBL4437388 | — | IC50 | = | 9170.0 | nM | 5.04 |
| CHEMBL4526752 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL4566524 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4553483 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL4441455 | — | IC50 | = | 31100.0 | nM | 4.51 |
| CHEMBL4459356 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4588852 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL36 | PYRIMETHAMINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL4542001 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL22148 | — | IC50 | > | 50000.0 | nM | - |