Assay Detail
Binding
CHEMBL1038911
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DHFR in presence of variable DHFA level by enzyme kinetics assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 5.94 | 10.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 10.11 |
| CHEMBL606039 | — | — | 1 | 6.30 |
| CHEMBL603198 | — | — | 1 | 6.19 |
| CHEMBL595757 | — | — | 1 | 6.11 |
| CHEMBL594810 | — | — | 1 | 6.08 |
| CHEMBL603849 | — | — | 1 | 5.96 |
| CHEMBL594320 | — | — | 1 | 5.89 |
| CHEMBL610181 | — | — | 1 | 5.80 |
| CHEMBL595497 | — | — | 1 | 5.80 |
| CHEMBL605413 | — | — | 1 | 5.60 |
| CHEMBL604879 | — | — | 1 | 5.37 |
| CHEMBL594339 | — | — | 1 | 5.34 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.31 |
| CHEMBL606362 | — | — | 1 | 5.28 |
| CHEMBL593154 | — | — | 1 | 4.96 |
| CHEMBL594790 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | Ki | = | 0.077 | nM | 10.11 |
| CHEMBL606039 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL603198 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL595757 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL594810 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL603849 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL594320 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL610181 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL595497 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL605413 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL604879 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL594339 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL606362 | — | Ki | = | 5300.0 | nM | 5.28 |
| CHEMBL593154 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL594790 | — | Ki | = | 12000.0 | nM | 4.92 |