Assay Detail
Functional
CHEMBL4410615
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Antimalarial activity against Plasmodium falciparum TM4/8.2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 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 | 6.37 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447272 | — | — | 1 | 7.37 |
| CHEMBL4590684 | — | — | 1 | 7.32 |
| CHEMBL4461699 | — | — | 1 | 7.31 |
| CHEMBL4462327 | — | — | 1 | 7.29 |
| CHEMBL4586252 | — | — | 1 | 7.28 |
| CHEMBL4588852 | — | — | 1 | 7.24 |
| CHEMBL4546946 | — | — | 1 | 7.15 |
| CHEMBL4452609 | — | — | 1 | 7.15 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 7.10 |
| CHEMBL4553483 | — | — | 1 | 6.89 |
| CHEMBL4565928 | — | — | 1 | 6.77 |
| CHEMBL4558959 | — | — | 1 | 6.47 |
| CHEMBL4526752 | — | — | 1 | 6.44 |
| CHEMBL4467953 | — | — | 1 | 6.42 |
| CHEMBL4437388 | — | — | 1 | 6.37 |
| CHEMBL4515405 | — | — | 1 | 6.19 |
| CHEMBL4444614 | — | — | 1 | 6.15 |
| CHEMBL22148 | — | — | 1 | 6.14 |
| CHEMBL4542001 | — | — | 1 | 5.90 |
| CHEMBL4468791 | — | — | 1 | 5.75 |
| CHEMBL4459902 | — | — | 1 | 5.71 |
| CHEMBL4441455 | — | — | 1 | 5.28 |
| CHEMBL4566524 | — | — | 1 | 5.22 |
| CHEMBL4456065 | — | — | 1 | 5.20 |
| CHEMBL4557136 | — | — | 1 | 5.17 |
| CHEMBL4459356 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447272 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4590684 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4461699 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4462327 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4586252 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4588852 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4546946 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4452609 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4553483 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4565928 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4558959 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4526752 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4467953 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4437388 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4515405 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4444614 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL22148 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4542001 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4468791 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4459902 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL4441455 | — | IC50 | = | 5240.0 | nM | 5.28 |
| CHEMBL4566524 | — | IC50 | = | 6010.0 | nM | 5.22 |
| CHEMBL4456065 | — | IC50 | = | 6250.0 | nM | 5.20 |
| CHEMBL4557136 | — | IC50 | = | 6730.0 | nM | 5.17 |
| CHEMBL4459356 | — | IC50 | = | 52600.0 | nM | 4.28 |