Assay Detail
Binding
CHEMBL665590
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Inhibitory activity against Toxoplasma gondii dihydrofolate reductase
66
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Toxoplasma gondii |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL2425) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 66 | 6.92 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL283518 | — | — | 1 | 8.57 |
| CHEMBL23532 | — | — | 1 | 8.57 |
| CHEMBL279680 | — | — | 1 | 8.54 |
| CHEMBL23569 | — | — | 1 | 8.46 |
| CHEMBL22623 | — | — | 1 | 8.40 |
| CHEMBL23382 | — | — | 1 | 8.14 |
| CHEMBL284544 | — | — | 1 | 8.10 |
| CHEMBL279983 | — | — | 1 | 8.00 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL23021 | — | — | 1 | 7.85 |
| CHEMBL279705 | — | — | 1 | 7.82 |
| CHEMBL23220 | — | — | 1 | 7.80 |
| CHEMBL23383 | — | — | 1 | 7.80 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.77 |
| CHEMBL23963 | — | — | 1 | 7.75 |
| CHEMBL279679 | — | — | 1 | 7.66 |
| CHEMBL281648 | — | — | 1 | 7.66 |
| CHEMBL23713 | — | — | 1 | 7.64 |
| CHEMBL282948 | — | — | 1 | 7.58 |
| CHEMBL23374 | — | — | 1 | 7.58 |
| CHEMBL23211 | — | — | 1 | 7.57 |
| CHEMBL281803 | — | — | 1 | 7.55 |
| CHEMBL23844 | — | — | 1 | 7.54 |
| CHEMBL23584 | — | — | 1 | 7.52 |
| CHEMBL23244 | — | — | 1 | 7.52 |
| CHEMBL23416 | — | — | 1 | 7.50 |
| CHEMBL23227 | — | — | 1 | 7.48 |
| CHEMBL291239 | — | — | 1 | 7.47 |
| CHEMBL23076 | — | — | 1 | 7.42 |
| CHEMBL23705 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL283518 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL23532 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL279680 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL23569 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL22623 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL23382 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL284544 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL279983 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL23021 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL279705 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL23220 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL23383 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL23963 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL279679 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL281648 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL23713 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL282948 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL23374 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL23211 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL281803 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL23844 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL23584 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL23244 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL23416 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL23227 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL291239 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL23076 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL23705 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL24344 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL23911 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL23272 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL26006 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL23092 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL24007 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL22677 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL281131 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL23919 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL277217 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL23288 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL23454 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL22924 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL22543 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL23867 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL23492 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL23560 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL22672 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL279243 | — | IC50 | = | 770.0 | nM | 6.11 |