Assay Detail
Binding
CHEMBL746911
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Inhibitory constant for F31A/F34A murine dihydrofolate reductase (DHFR)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Dihydrofolate reductase mutant with exceptional resistance to methotrexate but not to trimetrexate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.46 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 9.09 |
| CHEMBL18155 | — | — | 1 | 7.59 |
| CHEMBL406356 | — | — | 1 | 6.67 |
| CHEMBL328499 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL18155 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL406356 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL328499 | — | Ki | = | 333.0 | nM | 6.48 |