Assay Detail
Binding
CHEMBL664919
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Inhibitory activity against Dihydrohydrofolate reductase(DHFR) of Toxoplasma gondii
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Toxoplasma gondii |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL2425) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.72 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL33921 | — | — | 1 | 8.08 |
| CHEMBL48189 | — | — | 1 | 7.75 |
| CHEMBL32113 | — | — | 1 | 7.55 |
| CHEMBL288350 | — | — | 1 | 7.52 |
| CHEMBL37334 | — | — | 1 | 7.50 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.37 |
| CHEMBL301769 | — | — | 1 | 7.37 |
| CHEMBL285279 | — | — | 1 | 7.24 |
| CHEMBL33922 | — | — | 1 | 7.14 |
| CHEMBL34823 | — | — | 1 | 7.01 |
| CHEMBL37520 | — | — | 1 | 6.96 |
| CHEMBL36310 | — | — | 1 | 6.75 |
| CHEMBL48203 | — | — | 1 | 6.72 |
| CHEMBL48296 | — | — | 1 | 6.62 |
| CHEMBL49246 | — | — | 1 | 6.51 |
| CHEMBL48963 | — | — | 1 | 6.33 |
| CHEMBL35437 | — | — | 1 | 6.30 |
| CHEMBL288647 | — | — | 1 | 6.22 |
| CHEMBL50379 | — | — | 1 | 6.11 |
| CHEMBL50597 | — | — | 1 | 6.07 |
| CHEMBL48648 | — | — | 1 | 5.96 |
| CHEMBL35080 | — | — | 1 | 5.80 |
| CHEMBL17323 | — | — | 1 | 5.77 |
| CHEMBL290806 | — | — | 1 | 5.70 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL33921 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL48189 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL32113 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL288350 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL37334 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL301769 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL285279 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL33922 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL34823 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL37520 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL36310 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL48203 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL48296 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL49246 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL48963 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL35437 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL288647 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL50379 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL50597 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL48648 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL35080 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL17323 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL290806 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 2800.0 | nM | 5.55 |