Assay Detail
Binding
CHEMBL665356
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Inhibition of recombinant Dihydrofolate reductase from Leishmania major.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Leishmania major |
| 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 | 20 | 6.73 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135935 | — | — | 1 | 7.32 |
| CHEMBL274031 | — | — | 1 | 7.19 |
| CHEMBL344592 | — | — | 1 | 7.03 |
| CHEMBL31235 | — | — | 1 | 7.01 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 6.92 |
| CHEMBL343127 | — | — | 1 | 6.89 |
| CHEMBL343271 | — | — | 1 | 6.89 |
| CHEMBL137305 | — | — | 1 | 6.85 |
| CHEMBL31946 | — | — | 1 | 6.82 |
| CHEMBL137448 | — | — | 1 | 6.81 |
| CHEMBL334919 | — | — | 1 | 6.80 |
| CHEMBL31547 | — | — | 1 | 6.77 |
| CHEMBL285209 | — | — | 1 | 6.66 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 6.60 |
| CHEMBL18967 | — | — | 1 | 6.52 |
| CHEMBL326989 | — | — | 1 | 6.48 |
| CHEMBL137641 | — | — | 1 | 6.44 |
| CHEMBL138230 | — | — | 1 | 6.43 |
| CHEMBL30734 | — | — | 1 | 6.12 |
| CHEMBL334695 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135935 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL274031 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL344592 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL31235 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL343127 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL343271 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL137305 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL31946 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL137448 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL334919 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL31547 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL285209 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL36 | PYRIMETHAMINE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL18967 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL326989 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL137641 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL138230 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL30734 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL334695 | — | Ki | = | 750.0 | nM | 6.12 |