Assay Detail
Binding
CHEMBL889604
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Inhibition of human DHFR
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design and synthesis of classical and nonclassical 6-arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as antifolates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.67 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.66 |
| CHEMBL438664 | — | — | 1 | 7.18 |
| CHEMBL227063 | — | — | 1 | 5.85 |
| CHEMBL388120 | — | — | 1 | 5.85 |
| CHEMBL226954 | — | — | 1 | 5.57 |
| CHEMBL227007 | — | — | 1 | 5.55 |
| CHEMBL388121 | — | — | 1 | 5.54 |
| CHEMBL226952 | — | — | 1 | 5.54 |
| CHEMBL389887 | — | — | 1 | 5.24 |
| CHEMBL227009 | — | — | 1 | 5.24 |
| CHEMBL226953 | — | — | 1 | 5.22 |
| CHEMBL389686 | — | — | 1 | 4.75 |
| CHEMBL227064 | — | — | 1 | 4.50 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
| CHEMBL227010 | — | — | 1 | - |
| CHEMBL227008 | — | — | 1 | - |
| CHEMBL226955 | — | — | 1 | - |
| CHEMBL387901 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL438664 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL227063 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL388120 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL226954 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL227007 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL388121 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL226952 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL389887 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL227009 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL226953 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL389686 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL227064 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 680000.0 | nM | - |
| CHEMBL227010 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL227008 | — | IC50 | > | 28000.0 | nM | - |
| CHEMBL226955 | — | IC50 | > | 31000.0 | nM | - |
| CHEMBL387901 | — | IC50 | > | 31000.0 | nM | - |