Assay Detail
Binding
CHEMBL666700
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Inhibition Dihydrohydrofolate reductase(DHFR) of 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
Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.43 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.48 |
| CHEMBL37334 | — | — | 1 | 5.66 |
| CHEMBL285279 | — | — | 1 | 5.50 |
| CHEMBL34823 | — | — | 1 | 5.40 |
| CHEMBL33921 | — | — | 1 | 5.39 |
| CHEMBL288350 | — | — | 1 | 5.34 |
| CHEMBL37520 | — | — | 1 | 5.34 |
| CHEMBL35437 | — | — | 1 | 5.21 |
| CHEMBL35080 | — | — | 1 | 4.85 |
| CHEMBL288647 | — | — | 1 | 4.72 |
| CHEMBL290806 | — | — | 1 | 4.68 |
| CHEMBL33922 | — | — | 1 | 4.60 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL37334 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL285279 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL34823 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL33921 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL288350 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL37520 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL35437 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL35080 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL288647 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL290806 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL33922 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 180000.0 | nM | - |