Assay Detail
Binding
CHEMBL665601
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Toxoplasma gondii Dihydrofolate reductase
12
Total Activities
12
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
Synthesis and biological activities of tricyclic conformationally restricted tetrahydropyrido annulated furo[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.68 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.85 |
| CHEMBL17383 | — | — | 1 | 6.16 |
| CHEMBL30403 | — | — | 1 | 5.85 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.57 |
| CHEMBL287579 | — | — | 1 | 4.88 |
| CHEMBL278515 | — | — | 1 | 4.70 |
| CHEMBL418214 | — | — | 1 | 4.67 |
| CHEMBL31273 | — | — | 1 | 4.65 |
| CHEMBL281962 | — | — | 1 | 4.50 |
| CHEMBL287240 | — | — | 1 | - |
| CHEMBL284960 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL17383 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL30403 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL287579 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL278515 | — | IC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL418214 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL31273 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL281962 | — | IC50 | = | 31700.0 | nM | 4.50 |
| CHEMBL287240 | — | IC50 | > | 35000.0 | nM | - |
| CHEMBL284960 | — | IC50 | > | 20400.0 | nM | - |