Assay Detail
Binding
CHEMBL4410606
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Competitive inhibition of wild type Plasmodium falciparum dihydrofolate reductase expressed in Escherichia coli BL21(DE3)pLysS using dihydrofolate as substrate in presence of NADPH by UV-vis spectrophotometry analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| Ki | 27 | 9.21 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4553483 | — | — | 1 | 9.68 |
| CHEMBL4565928 | — | — | 1 | 9.62 |
| CHEMBL4590684 | — | — | 1 | 9.60 |
| CHEMBL4452609 | — | — | 1 | 9.59 |
| CHEMBL4526752 | — | — | 1 | 9.55 |
| CHEMBL4586252 | — | — | 1 | 9.54 |
| CHEMBL4467953 | — | — | 1 | 9.52 |
| CHEMBL4447272 | — | — | 1 | 9.43 |
| CHEMBL4558959 | — | — | 1 | 9.42 |
| CHEMBL4461699 | — | — | 1 | 9.36 |
| CHEMBL4462327 | — | — | 1 | 9.35 |
| CHEMBL4588852 | — | — | 1 | 9.30 |
| CHEMBL4546946 | — | — | 1 | 9.26 |
| CHEMBL4437388 | — | — | 1 | 9.26 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 9.22 |
| CHEMBL4459902 | — | — | 1 | 9.19 |
| CHEMBL4444614 | — | — | 1 | 9.18 |
| CHEMBL278847 | — | — | 1 | 9.10 |
| CHEMBL4566524 | — | — | 1 | 9.06 |
| CHEMBL4515405 | — | — | 1 | 9.02 |
| CHEMBL4459356 | — | — | 1 | 8.99 |
| CHEMBL4542001 | — | — | 1 | 8.93 |
| CHEMBL4441455 | — | — | 1 | 8.83 |
| CHEMBL4468791 | — | — | 1 | 8.81 |
| CHEMBL4557136 | — | — | 1 | 8.75 |
| CHEMBL22148 | — | — | 1 | 8.64 |
| CHEMBL4456065 | — | — | 1 | 8.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4553483 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL4565928 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL4590684 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL4452609 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL4526752 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL4586252 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL4467953 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4447272 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL4558959 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL4461699 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL4462327 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL4588852 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4546946 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL4437388 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL36 | PYRIMETHAMINE | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4459902 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL4444614 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL278847 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4566524 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL4515405 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL4459356 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL4542001 | — | Ki | = | 1.17 | nM | 8.93 |
| CHEMBL4441455 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL4468791 | — | Ki | = | 1.55 | nM | 8.81 |
| CHEMBL4557136 | — | Ki | = | 1.78 | nM | 8.75 |
| CHEMBL22148 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4456065 | — | Ki | = | 3.76 | nM | 8.43 |