Assay Detail
Binding
CHEMBL4338382
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Inhibition of Trypanosoma brucei rhodesiense rhodesain expressed in Pichia pastoris assessed as inhibition constant measured for 30 mins using Cbz-Phe-Arg-AMC as substrate by fluorescence assay
15
Total Activities
15
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
Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 9.51 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4436812 | — | — | 1 | 10.82 |
| CHEMBL4453415 | — | — | 1 | 10.64 |
| CHEMBL4584291 | — | — | 1 | 10.54 |
| CHEMBL4437914 | — | — | 1 | 10.47 |
| CHEMBL4459413 | — | — | 1 | 9.30 |
| CHEMBL4456010 | — | — | 1 | 9.13 |
| CHEMBL4456727 | — | — | 1 | 8.74 |
| CHEMBL4454883 | — | — | 1 | 8.68 |
| CHEMBL4464737 | — | — | 1 | 8.51 |
| CHEMBL4438444 | — | — | 1 | 8.26 |
| CHEMBL4515298 | — | — | 1 | - |
| CHEMBL4475066 | — | — | 1 | - |
| CHEMBL4587965 | — | — | 1 | - |
| CHEMBL4566436 | — | — | 1 | - |
| CHEMBL4441635 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4436812 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL4453415 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL4584291 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL4437914 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL4459413 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4456010 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL4456727 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4454883 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4464737 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL4438444 | — | Ki | = | 5.54 | nM | 8.26 |
| CHEMBL4515298 | — | Ki | = | 0.003 | nM | - |
| CHEMBL4475066 | — | Ki | = | 0.0011 | nM | - |
| CHEMBL4587965 | — | Ki | = | 0.0044 | nM | - |
| CHEMBL4566436 | — | Ki | = | 0.0006 | nM | - |
| CHEMBL4441635 | — | Ki | = | 0.0076 | nM | - |