Assay Detail
Binding
CHEMBL661507
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Inhibitory activity against dihydrofolate reductase (DHFR) from Toxoplasma gondii
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
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.83 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337603 | — | — | 1 | 9.06 |
| CHEMBL140940 | — | — | 1 | 8.66 |
| CHEMBL139485 | — | — | 1 | 8.12 |
| CHEMBL141160 | — | — | 1 | 8.07 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.77 |
| CHEMBL137981 | — | — | 1 | 7.72 |
| CHEMBL141698 | — | — | 1 | 7.39 |
| CHEMBL137844 | — | — | 1 | 7.35 |
| CHEMBL142081 | — | — | 1 | 7.24 |
| CHEMBL337746 | — | — | 1 | 6.68 |
| CHEMBL139188 | — | — | 1 | 6.52 |
| CHEMBL140705 | — | — | 1 | 6.34 |
| CHEMBL141808 | — | — | 1 | 6.31 |
| CHEMBL141585 | — | — | 1 | 6.17 |
| CHEMBL141260 | — | — | 1 | 6.14 |
| CHEMBL138252 | — | — | 1 | 6.08 |
| CHEMBL140597 | — | — | 1 | 6.03 |
| CHEMBL342654 | — | — | 1 | 6.00 |
| CHEMBL138419 | — | — | 1 | 5.96 |
| CHEMBL334456 | — | — | 1 | 5.68 |
| CHEMBL138452 | — | — | 1 | 5.62 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.57 |
| CHEMBL141218 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337603 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL140940 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL139485 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL141160 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL137981 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL141698 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL137844 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL142081 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL337746 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL139188 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL140705 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL141808 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL141585 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL141260 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL138252 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL140597 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL342654 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL138419 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL334456 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL138452 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL141218 | — | IC50 | = | 2800.0 | nM | 5.55 |