Assay Detail
Binding
CHEMBL884432
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Inhibition of dihydrofolate reductase from pneumocystis carinii.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of 2,4-diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase and as antiopportunistic infection and antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.38 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50514 | — | — | 1 | 7.89 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.51 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.38 |
| CHEMBL22924 | — | — | 1 | 7.16 |
| CHEMBL32113 | — | — | 1 | 7.08 |
| CHEMBL23532 | — | — | 1 | 7.07 |
| CHEMBL147828 | — | — | 1 | 6.88 |
| CHEMBL149099 | — | — | 1 | 6.71 |
| CHEMBL142741 | — | — | 1 | 6.62 |
| CHEMBL147870 | — | — | 1 | 6.60 |
| CHEMBL358351 | — | — | 1 | 6.46 |
| CHEMBL149301 | — | — | 1 | 6.37 |
| CHEMBL145979 | — | — | 1 | 6.36 |
| CHEMBL356279 | — | — | 1 | 6.28 |
| CHEMBL23288 | — | — | 1 | 5.82 |
| CHEMBL146039 | — | — | 1 | 5.70 |
| CHEMBL358003 | — | — | 1 | 5.65 |
| CHEMBL424135 | — | — | 1 | 5.21 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.92 |
| CHEMBL146622 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50514 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL22924 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL32113 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL23532 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL147828 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL149099 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL142741 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL147870 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL358351 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL149301 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL145979 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL356279 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL23288 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL146039 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL358003 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL424135 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL146622 | — | IC50 | = | 100000.0 | nM | 4.00 |