Assay Detail
Binding
CHEMBL1038912
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat liver DHFR by enzyme kinetics assay in presence of variable DHFA level
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.88 | 10.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 10.14 |
| CHEMBL603849 | — | — | 1 | 6.00 |
| CHEMBL606039 | — | — | 1 | 5.96 |
| CHEMBL594320 | — | — | 1 | 5.96 |
| CHEMBL603198 | — | — | 1 | 5.96 |
| CHEMBL594810 | — | — | 1 | 5.89 |
| CHEMBL595757 | — | — | 1 | 5.85 |
| CHEMBL595497 | — | — | 1 | 5.80 |
| CHEMBL604879 | — | — | 1 | 5.50 |
| CHEMBL605413 | — | — | 1 | 5.48 |
| CHEMBL594339 | — | — | 1 | 5.40 |
| CHEMBL606362 | — | — | 1 | 5.38 |
| CHEMBL610181 | — | — | 1 | 5.34 |
| CHEMBL593154 | — | — | 1 | 5.33 |
| CHEMBL594790 | — | — | 1 | 5.30 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL603849 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL606039 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL594320 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL603198 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL594810 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL595757 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL595497 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL604879 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL605413 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL594339 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL606362 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL610181 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL593154 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL594790 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 14300.0 | nM | 4.84 |