Assay Detail
Binding
CHEMBL829464
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Inhibition of human dihydrofolate reductase at 37 degree C pH 7.4
7
Total Activities
7
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
Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.81 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.66 |
| CHEMBL323565 | — | — | 1 | 6.00 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 5.64 |
| CHEMBL223279 | — | — | 1 | 5.05 |
| CHEMBL193275 | — | — | 1 | 4.68 |
| CHEMBL192632 | — | — | 1 | - |
| CHEMBL365307 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL323565 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL223279 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL193275 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL192632 | — | IC50 | > | 24000.0 | nM | - |
| CHEMBL365307 | — | IC50 | > | 20000.0 | nM | - |