Assay Detail
Binding
CHEMBL665616
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Inhibitory activity against Toxoplasma gondii dihydrofolate reductase (in 90 uM dihydrofolic acid)
24
Total Activities
24
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
2,4-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.63 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32113 | — | — | 1 | 8.20 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.85 |
| CHEMBL32190 | — | — | 1 | 7.85 |
| CHEMBL36245 | — | — | 1 | 7.68 |
| CHEMBL35222 | — | — | 1 | 7.58 |
| CHEMBL33038 | — | — | 1 | 7.50 |
| CHEMBL32583 | — | — | 1 | 6.71 |
| CHEMBL32754 | — | — | 1 | 6.64 |
| CHEMBL32708 | — | — | 1 | 6.51 |
| CHEMBL33208 | — | — | 1 | 6.46 |
| CHEMBL32220 | — | — | 1 | 6.42 |
| CHEMBL280378 | EPIROPRIM | 2.0 | 1 | 6.33 |
| CHEMBL284849 | — | — | 1 | 6.32 |
| CHEMBL286700 | — | — | 1 | 6.28 |
| CHEMBL35569 | — | — | 1 | 6.17 |
| CHEMBL33357 | — | — | 1 | 6.15 |
| CHEMBL32769 | — | — | 1 | 6.14 |
| CHEMBL34337 | — | — | 1 | 6.04 |
| CHEMBL32635 | — | — | 1 | 6.01 |
| CHEMBL32266 | — | — | 1 | 5.92 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.57 |
| CHEMBL33187 | — | — | 1 | 5.43 |
| CHEMBL33136 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32113 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL32190 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL36245 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL35222 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL33038 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL32583 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL32754 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL32708 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL33208 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL32220 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL280378 | EPIROPRIM | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL284849 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL286700 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL35569 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL33357 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL32769 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL34337 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL32635 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL32266 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL33187 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL33136 | — | IC50 | = | 4450.0 | nM | 5.35 |