Assay Detail
Binding
CHEMBL669873
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Inhibition of human recombinant Dihydrofolate reductase enzyme
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.59 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 10.60 |
| CHEMBL369258 | — | — | 1 | 10.00 |
| CHEMBL170760 | — | — | 1 | 10.00 |
| CHEMBL171765 | — | — | 1 | 10.00 |
| CHEMBL170837 | — | — | 1 | 9.70 |
| CHEMBL352960 | — | — | 1 | 9.70 |
| CHEMBL170758 | — | — | 1 | 9.52 |
| CHEMBL424170 | — | — | 1 | 9.40 |
| CHEMBL171494 | — | — | 1 | 9.40 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.85 |
| CHEMBL318721 | — | — | 1 | 8.35 |
| CHEMBL353621 | — | — | 1 | 8.22 |
| CHEMBL173617 | — | — | 1 | 8.19 |
| CHEMBL170144 | — | — | 1 | 8.00 |
| CHEMBL353161 | — | — | 1 | 8.00 |
| CHEMBL353763 | — | — | 1 | 7.62 |
| CHEMBL170900 | — | — | 1 | 7.54 |
| CHEMBL171629 | — | — | 1 | 7.52 |
| CHEMBL353929 | — | — | 1 | 7.06 |
| CHEMBL174414 | — | — | 1 | 6.64 |
| CHEMBL353764 | — | — | 1 | 6.00 |
| CHEMBL171305 | — | — | 1 | - |
| CHEMBL170654 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL369258 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL170760 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL171765 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL170837 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL352960 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL170758 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL424170 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL171494 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL119 | TRIMETREXATE | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL318721 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL353621 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL173617 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL170144 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL353161 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL353763 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL170900 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL171629 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL353929 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL174414 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL353764 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL171305 | — | Ki | < | 2.0 | nM | - |
| CHEMBL170654 | — | Ki | < | 2.0 | nM | - |