Assay Detail
Binding
CHEMBL663138
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Inhibitory activity against recombinant sf dihydrofolate reductase(in 50 uM dihydrofolic acid)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Enterococcus faecium |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 7 | 7.86 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.66 |
| CHEMBL33815 | — | — | 1 | 8.66 |
| CHEMBL33045 | — | — | 1 | 8.00 |
| CHEMBL32708 | — | — | 1 | 7.82 |
| CHEMBL32113 | — | — | 1 | 7.55 |
| CHEMBL33208 | — | — | 1 | 7.29 |
| CHEMBL32266 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL33815 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL33045 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL32708 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL32113 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL33208 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL32266 | — | IC50 | = | 86.0 | nM | 7.07 |