Assay Detail
Binding
CHEMBL665621
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Dihydrofolate reductase from humans.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.83 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31946 | — | — | 1 | 8.44 |
| CHEMBL326989 | — | — | 1 | 8.19 |
| CHEMBL137305 | — | — | 1 | 8.15 |
| CHEMBL137448 | — | — | 1 | 8.07 |
| CHEMBL334919 | — | — | 1 | 8.06 |
| CHEMBL18967 | — | — | 1 | 8.02 |
| CHEMBL31547 | — | — | 1 | 8.01 |
| CHEMBL343271 | — | — | 1 | 8.01 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 8.00 |
| CHEMBL343127 | — | — | 1 | 7.98 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 7.96 |
| CHEMBL274031 | — | — | 1 | 7.96 |
| CHEMBL344592 | — | — | 1 | 7.89 |
| CHEMBL135935 | — | — | 1 | 7.72 |
| CHEMBL31235 | — | — | 1 | 7.62 |
| CHEMBL137641 | — | — | 1 | 7.44 |
| CHEMBL334695 | — | — | 1 | 7.28 |
| CHEMBL138230 | — | — | 1 | 7.12 |
| CHEMBL285209 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31946 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL326989 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL137305 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL137448 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL334919 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL18967 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL31547 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL343271 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL343127 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL36 | PYRIMETHAMINE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL274031 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL344592 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL135935 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL31235 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL137641 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL334695 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL138230 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL285209 | — | Ki | = | 131.0 | nM | 6.88 |