Assay Detail
Binding
CHEMBL665443
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Inhibitory activity against rat liver dihydrofolate reductase (in 90 uM dihydrofolic acid)
24
Total Activities
24
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-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.39 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.60 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL35222 | — | — | 1 | 7.52 |
| CHEMBL32190 | — | — | 1 | 7.48 |
| CHEMBL32113 | — | — | 1 | 7.24 |
| CHEMBL36245 | — | — | 1 | 7.14 |
| CHEMBL33038 | — | — | 1 | 6.85 |
| CHEMBL32635 | — | — | 1 | 6.62 |
| CHEMBL33136 | — | — | 1 | 6.55 |
| CHEMBL32708 | — | — | 1 | 6.46 |
| CHEMBL33357 | — | — | 1 | 6.43 |
| CHEMBL32220 | — | — | 1 | 6.37 |
| CHEMBL284849 | — | — | 1 | 5.96 |
| CHEMBL32754 | — | — | 1 | 5.92 |
| CHEMBL32583 | — | — | 1 | 5.90 |
| CHEMBL34337 | — | — | 1 | 5.85 |
| CHEMBL32769 | — | — | 1 | 5.82 |
| CHEMBL286700 | — | — | 1 | 5.68 |
| CHEMBL33187 | — | — | 1 | 5.54 |
| CHEMBL35569 | — | — | 1 | 5.49 |
| CHEMBL33208 | — | — | 1 | 5.48 |
| CHEMBL32266 | — | — | 1 | 5.47 |
| CHEMBL280378 | EPIROPRIM | 2.0 | 1 | 4.14 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL35222 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL32190 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL32113 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL36245 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL33038 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL32635 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL33136 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL32708 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL33357 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL32220 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL284849 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL32754 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL32583 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL34337 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL32769 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL286700 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL33187 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL35569 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL33208 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL32266 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL280378 | EPIROPRIM | IC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 133000.0 | nM | - |