Assay Detail
Binding
CHEMBL668777
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Inhibition of Dihydrofolate reductase of rat liver
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological activities of tricyclic conformationally restricted tetrahydropyrido annulated furo[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.59 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.52 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL278515 | — | — | 1 | 6.37 |
| CHEMBL17383 | — | — | 1 | 5.89 |
| CHEMBL30403 | — | — | 1 | 4.82 |
| CHEMBL31273 | — | — | 1 | 4.69 |
| CHEMBL284960 | — | — | 1 | 4.64 |
| CHEMBL287579 | — | — | 1 | 4.29 |
| CHEMBL281962 | — | — | 1 | 4.09 |
| CHEMBL418214 | — | — | 1 | 4.07 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
| CHEMBL287240 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL278515 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL17383 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL30403 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL31273 | — | IC50 | = | 20600.0 | nM | 4.69 |
| CHEMBL284960 | — | IC50 | = | 22800.0 | nM | 4.64 |
| CHEMBL287579 | — | IC50 | = | 50900.0 | nM | 4.29 |
| CHEMBL281962 | — | IC50 | = | 81200.0 | nM | 4.09 |
| CHEMBL418214 | — | IC50 | = | 85800.0 | nM | 4.07 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 133000.0 | nM | - |
| CHEMBL287240 | — | IC50 | > | 35000.0 | nM | - |