Assay Detail
Binding
CHEMBL867007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human DHFR
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
Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.23 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.66 |
| CHEMBL371860 | — | — | 1 | 6.38 |
| CHEMBL225180 | — | — | 1 | 5.68 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 5.18 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | - |
| CHEMBL389051 | — | — | 1 | - |
| CHEMBL202337 | — | — | 1 | - |
| CHEMBL436761 | — | — | 1 | - |
| CHEMBL369906 | — | — | 1 | - |
| CHEMBL383829 | — | — | 1 | - |
| CHEMBL370116 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL371860 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL225180 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL225071 | RALTITREXED | IC50 | - | — | - | |
| CHEMBL389051 | — | IC50 | - | — | - | |
| CHEMBL202337 | — | IC50 | - | — | - | |
| CHEMBL436761 | — | IC50 | - | — | - | |
| CHEMBL369906 | — | IC50 | - | — | - | |
| CHEMBL383829 | — | IC50 | - | — | - | |
| CHEMBL370116 | — | IC50 | - | — | - |