Assay Detail
Binding
CHEMBL4049094
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Trypanosoma brucei rhodesiense rhodesain using Cbz-Phe-Arg-AMC as substrate by fluorimetric method
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei rhodesiense |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.87 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4073014 | — | — | 1 | 8.70 |
| CHEMBL4080286 | — | — | 1 | 8.54 |
| CHEMBL4099905 | — | — | 1 | 8.52 |
| CHEMBL4064430 | — | — | 1 | 8.40 |
| CHEMBL4093712 | — | — | 1 | 8.15 |
| CHEMBL4086533 | — | — | 1 | 8.13 |
| CHEMBL4102966 | — | — | 1 | 8.13 |
| CHEMBL4078688 | — | — | 1 | 8.13 |
| CHEMBL4065096 | — | — | 1 | 8.13 |
| CHEMBL4082483 | — | — | 1 | 8.13 |
| CHEMBL4104507 | — | — | 1 | 8.13 |
| CHEMBL4084048 | — | — | 1 | 8.05 |
| CHEMBL4094298 | — | — | 1 | 8.05 |
| CHEMBL4096787 | — | — | 1 | 8.00 |
| CHEMBL4093144 | — | — | 1 | 7.96 |
| CHEMBL4095566 | — | — | 1 | 7.92 |
| CHEMBL4060895 | — | — | 1 | 7.85 |
| CHEMBL4083441 | — | — | 1 | 7.80 |
| CHEMBL4099235 | — | — | 1 | 7.80 |
| CHEMBL4081905 | — | — | 1 | 7.77 |
| CHEMBL4075154 | — | — | 1 | 7.75 |
| CHEMBL4065829 | — | — | 1 | 7.75 |
| CHEMBL4078079 | — | — | 1 | 7.75 |
| CHEMBL4089084 | — | — | 1 | 7.72 |
| CHEMBL4093444 | — | — | 1 | 7.64 |
| CHEMBL4102031 | — | — | 1 | 7.64 |
| CHEMBL4069564 | — | — | 1 | 7.60 |
| CHEMBL4074099 | — | — | 1 | 7.51 |
| CHEMBL4065483 | — | — | 1 | 7.51 |
| CHEMBL4102351 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4073014 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4080286 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4099905 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4064430 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4093712 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4086533 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL4102966 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL4078688 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL4065096 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL4082483 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL4104507 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL4084048 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4094298 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4096787 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4093144 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4095566 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4060895 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4083441 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4099235 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4081905 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4075154 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4065829 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4078079 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4089084 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4093444 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4102031 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4069564 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4074099 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4065483 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4102351 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4081213 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4100863 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4101430 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL4085387 | — | Ki | = | 93.0 | nM | 7.03 |