Assay Detail
Binding
CHEMBL875029
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Inhibition of rat liver Dihydrofolate reductase
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
Novel 2,4-diamino-5-substituted-pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolate inhibitors of dihydrofolate reductases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.12 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 9.00 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.52 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL17232 | — | — | 1 | 7.36 |
| CHEMBL17873 | — | — | 1 | 4.84 |
| CHEMBL69681 | — | — | 1 | 4.25 |
| CHEMBL276734 | — | — | 1 | 4.23 |
| CHEMBL68673 | — | — | 1 | 4.20 |
| CHEMBL69363 | — | — | 1 | 4.16 |
| CHEMBL17323 | — | — | 1 | - |
| CHEMBL432136 | — | — | 1 | - |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
| CHEMBL68439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL17232 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL17873 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL69681 | — | IC50 | = | 56300.0 | nM | 4.25 |
| CHEMBL276734 | — | IC50 | = | 59300.0 | nM | 4.23 |
| CHEMBL68673 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL69363 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL17323 | — | IC50 | = | 156000.0 | nM | - |
| CHEMBL432136 | — | IC50 | > | 252000.0 | nM | - |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 133000.0 | nM | - |
| CHEMBL68439 | — | IC50 | = | 116000.0 | nM | - |