Assay Detail
Binding
CHEMBL669014
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Inhibition of partially purified dihydrofolate reductase (DHFR) from rat liver
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines: marked improvement in potency relative to trimethoprim and species selectivity relative to piritrexim.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.15 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL37696 | — | — | 1 | 5.58 |
| CHEMBL37520 | — | — | 1 | 5.41 |
| CHEMBL287481 | — | — | 1 | 4.96 |
| CHEMBL289904 | — | — | 1 | 4.92 |
| CHEMBL38332 | — | — | 1 | 4.92 |
| CHEMBL36310 | — | — | 1 | 4.92 |
| CHEMBL285448 | — | — | 1 | 4.77 |
| CHEMBL284851 | — | — | 1 | 4.54 |
| CHEMBL78648 | — | — | 1 | 4.52 |
| CHEMBL79890 | — | — | 1 | 4.36 |
| CHEMBL420384 | — | — | 1 | 4.07 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL37696 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL37520 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL287481 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL289904 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL38332 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL36310 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL285448 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL284851 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL78648 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL79890 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL420384 | — | IC50 | = | 86000.0 | nM | 4.07 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 130000.0 | nM | - |