Assay Detail
Binding
CHEMBL668274
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Inhibitory activity against recombinant human dihydrofolate reductase(in 50 uM dihydrofolic acid)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct 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 | 11 | 5.74 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.42 |
| CHEMBL33045 | — | — | 1 | 6.50 |
| CHEMBL35222 | — | — | 1 | 6.28 |
| CHEMBL33815 | — | — | 1 | 6.19 |
| CHEMBL33038 | — | — | 1 | 6.16 |
| CHEMBL36245 | — | — | 1 | 5.54 |
| CHEMBL286700 | — | — | 1 | 5.21 |
| CHEMBL32113 | — | — | 1 | 5.07 |
| CHEMBL32708 | — | — | 1 | 4.89 |
| CHEMBL33208 | — | — | 1 | 4.12 |
| CHEMBL32266 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL33045 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL35222 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL33815 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL33038 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL36245 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL286700 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL32113 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL32708 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL33208 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL32266 | — | IC50 | = | 160000.0 | nM | - |