Assay Detail
Binding
CHEMBL875142
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Inhibition of rat liver dihydrofolate reductase.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.71 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL323960 | — | — | 1 | 6.43 |
| CHEMBL104787 | — | — | 1 | 6.40 |
| CHEMBL317017 | — | — | 1 | 6.24 |
| CHEMBL325333 | — | — | 1 | 5.89 |
| CHEMBL326200 | — | — | 1 | 5.75 |
| CHEMBL108006 | — | — | 1 | 5.72 |
| CHEMBL107023 | — | — | 1 | 5.51 |
| CHEMBL323155 | — | — | 1 | 5.41 |
| CHEMBL107167 | — | — | 1 | 5.34 |
| CHEMBL322585 | — | — | 1 | 5.23 |
| CHEMBL104770 | — | — | 1 | 5.03 |
| CHEMBL320811 | — | — | 1 | 4.85 |
| CHEMBL322861 | — | — | 1 | 4.60 |
| CHEMBL104379 | — | — | 1 | 4.58 |
| CHEMBL322315 | — | — | 1 | 4.29 |
| CHEMBL104555 | — | — | 1 | 4.24 |
| CHEMBL321826 | — | — | 1 | - |
| CHEMBL107079 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL323960 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL104787 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL317017 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL325333 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL326200 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL108006 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL107023 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL323155 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL107167 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL322585 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL104770 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL320811 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL322861 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL104379 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL322315 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL104555 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL321826 | — | IC50 | > | 37000.0 | nM | - |
| CHEMBL107079 | — | IC50 | > | 100000.0 | nM | - |