Assay Detail
Binding
CHEMBL884367
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Inhibitory activity against rat liver dihydrofolate reductase.
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Nonclassical 2,4-diamino-8-deazafolate analogues as inhibitors of dihydrofolate reductases from rat liver, Pneumocystis carinii, and Toxoplasma gondii.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 7.29 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL301795 | — | — | 1 | 8.60 |
| CHEMBL57624 | — | — | 1 | 8.57 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL55012 | — | — | 1 | 8.29 |
| CHEMBL54538 | — | — | 1 | 8.14 |
| CHEMBL55727 | — | — | 1 | 8.14 |
| CHEMBL53872 | — | — | 1 | 8.12 |
| CHEMBL52953 | — | — | 1 | 7.82 |
| CHEMBL299174 | — | — | 1 | 7.80 |
| CHEMBL300603 | — | — | 1 | 7.77 |
| CHEMBL415962 | — | — | 1 | 7.75 |
| CHEMBL55063 | — | — | 1 | 7.62 |
| CHEMBL52688 | — | — | 1 | 7.58 |
| CHEMBL55049 | — | — | 1 | 7.50 |
| CHEMBL54792 | — | — | 1 | 7.46 |
| CHEMBL299140 | — | — | 1 | 7.40 |
| CHEMBL53420 | — | — | 1 | 7.36 |
| CHEMBL55191 | — | — | 1 | 7.33 |
| CHEMBL445359 | — | — | 1 | 7.32 |
| CHEMBL301105 | — | — | 1 | 7.30 |
| CHEMBL52930 | — | — | 1 | 7.28 |
| CHEMBL292427 | — | — | 1 | 7.27 |
| CHEMBL54732 | — | — | 1 | 7.24 |
| CHEMBL55928 | — | — | 1 | 7.22 |
| CHEMBL54399 | — | — | 1 | 7.17 |
| CHEMBL52777 | — | — | 1 | 7.14 |
| CHEMBL54913 | — | — | 1 | 7.09 |
| CHEMBL292143 | — | — | 1 | 7.07 |
| CHEMBL292634 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL301795 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL57624 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL55012 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL54538 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL55727 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL53872 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL52953 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL299174 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL300603 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL415962 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL55063 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL52688 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL55049 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL54792 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL299140 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL53420 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL55191 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL445359 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL301105 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL52930 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL292427 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL54732 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL55928 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL54399 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL52777 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL54913 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL292143 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL292634 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL52698 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL53318 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL53974 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL53165 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL54618 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL55656 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL55179 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL292212 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL52836 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL417746 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL54733 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL52947 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL296382 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL54523 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL23911 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL300886 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL51706 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL279243 | — | IC50 | = | 246000.0 | nM | - |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 130000.0 | nM | - |