Assay Detail
Binding
CHEMBL1026636
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Inhibition of rat liver dihydrofolate reductase
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.70 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL493717 | — | — | 1 | 8.39 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.36 |
| CHEMBL521672 | — | — | 1 | 8.32 |
| CHEMBL492895 | — | — | 1 | 8.28 |
| CHEMBL493718 | — | — | 1 | 8.19 |
| CHEMBL523004 | — | — | 1 | 8.02 |
| CHEMBL522678 | — | — | 1 | 7.84 |
| CHEMBL455012 | — | — | 1 | 7.80 |
| CHEMBL492896 | — | — | 1 | 7.77 |
| CHEMBL522543 | — | — | 1 | 7.72 |
| CHEMBL325434 | — | — | 1 | 7.58 |
| CHEMBL32113 | — | — | 1 | 7.24 |
| CHEMBL32708 | — | — | 1 | 6.46 |
| CHEMBL116816 | — | — | 1 | 4.96 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL493717 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL521672 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL492895 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL493718 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL523004 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL522678 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL455012 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL492896 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL522543 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL325434 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL32113 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL32708 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL116816 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 133000.0 | nM | - |