Assay Detail
Binding
CHEMBL926728
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Inhibition of Trypanosoma brucei cathepsin B-like cysteine protease
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cathepsin B-like cysteine protease (CHEMBL5832) ↗| Type | SINGLE PROTEIN |
| Organism | Trypanosoma brucei |
Publication
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 56 | 5.29 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254412 | — | — | 1 | 6.57 |
| CHEMBL252934 | — | — | 1 | 6.24 |
| CHEMBL400543 | — | — | 1 | 6.10 |
| CHEMBL400542 | — | — | 1 | 6.03 |
| CHEMBL254617 | — | — | 1 | 5.92 |
| CHEMBL400663 | — | — | 1 | 5.85 |
| CHEMBL399094 | — | — | 1 | 5.64 |
| CHEMBL254618 | — | — | 1 | 5.60 |
| CHEMBL252933 | — | — | 1 | 5.55 |
| CHEMBL400248 | — | — | 1 | 5.48 |
| CHEMBL251923 | — | — | 1 | 5.48 |
| CHEMBL254619 | — | — | 1 | 5.47 |
| CHEMBL255038 | — | — | 1 | 5.39 |
| CHEMBL255087 | — | — | 1 | 5.38 |
| CHEMBL255086 | — | — | 1 | 5.35 |
| CHEMBL398505 | — | — | 1 | 5.32 |
| CHEMBL252359 | — | — | 1 | 5.30 |
| CHEMBL400454 | — | — | 1 | 5.22 |
| CHEMBL400095 | — | — | 1 | 5.22 |
| CHEMBL252362 | — | — | 1 | 5.16 |
| CHEMBL399027 | — | — | 1 | 5.15 |
| CHEMBL252360 | — | — | 1 | 5.08 |
| CHEMBL254827 | — | — | 1 | 5.08 |
| CHEMBL402052 | — | — | 1 | 5.08 |
| CHEMBL253830 | — | — | 1 | 5.00 |
| CHEMBL255080 | — | — | 1 | 5.00 |
| CHEMBL399026 | — | — | 1 | 4.96 |
| CHEMBL429121 | — | — | 1 | 4.96 |
| CHEMBL252363 | — | — | 1 | 4.96 |
| CHEMBL400097 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254412 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL252934 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL400543 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL400542 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL254617 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL400663 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL399094 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL254618 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL252933 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL400248 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL251923 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL254619 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL255038 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL255087 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL255086 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL398505 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL252359 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL400454 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL400095 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL252362 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL399027 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL252360 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL254827 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL402052 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL255080 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL253830 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL399026 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL429121 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL252363 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL400097 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL254227 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL255079 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL400664 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL398708 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL252729 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL253611 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL252121 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL436637 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL400096 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL399513 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL398507 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL252158 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL252157 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL399095 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL252156 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL251959 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL251973 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL400522 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL398504 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL252361 | — | IC50 | > | 25000.0 | nM | - |