Assay Detail
Binding
CHEMBL884437
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In vitro inhibition of human dihydrofolate reductase (DHFR)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Side chain modified 5-deazafolate and 5-deazatetrahydrofolate analogues as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyltransferase inhibitors: synthesis and in vitro biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.22 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.57 |
| CHEMBL39175 | — | — | 1 | 6.40 |
| CHEMBL294973 | — | — | 1 | 5.89 |
| CHEMBL40850 | — | — | 1 | 5.33 |
| CHEMBL417696 | — | — | 1 | 4.92 |
| CHEMBL38902 | — | — | 1 | - |
| CHEMBL41459 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL39175 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL294973 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL40850 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL417696 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL38902 | — | IC50 | = | 220000.0 | nM | - |
| CHEMBL41459 | — | IC50 | = | 950000.0 | nM | - |