Assay Detail
Functional
CHEMBL3387686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antitrypanosomal activity against Trypanosoma brucei BSF427 expressing VSG118 infected in human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei |
| Cell Type | MRC5 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 48 | 7.87 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3357685 | ZELENIRSTAT | 2.0 | 1 | 9.40 |
| CHEMBL3357697 | — | — | 1 | 9.30 |
| CHEMBL3357699 | — | — | 1 | 9.22 |
| CHEMBL3358121 | — | — | 1 | 9.22 |
| CHEMBL3358120 | — | — | 1 | 9.22 |
| CHEMBL3358111 | — | — | 1 | 9.00 |
| CHEMBL3358114 | — | — | 1 | 9.00 |
| CHEMBL3358119 | — | — | 1 | 9.00 |
| CHEMBL3357702 | — | — | 1 | 8.70 |
| CHEMBL1230468 | — | — | 1 | 8.70 |
| CHEMBL3357695 | — | — | 1 | 8.70 |
| CHEMBL3357693 | — | — | 1 | 8.70 |
| CHEMBL3358122 | — | — | 1 | 8.70 |
| CHEMBL3357682 | — | — | 1 | 8.70 |
| CHEMBL3358113 | — | — | 1 | 8.52 |
| CHEMBL3358117 | — | — | 1 | 8.52 |
| CHEMBL3358123 | — | — | 1 | 8.40 |
| CHEMBL3358125 | — | — | 1 | 8.40 |
| CHEMBL3357684 | — | — | 1 | 8.30 |
| CHEMBL3358127 | — | — | 1 | 8.30 |
| CHEMBL3358124 | — | — | 1 | 8.22 |
| CHEMBL3357703 | — | — | 1 | 8.22 |
| CHEMBL3357686 | — | — | 1 | 8.22 |
| CHEMBL3357700 | — | — | 1 | 8.05 |
| CHEMBL3358118 | — | — | 1 | 8.00 |
| CHEMBL3357706 | — | — | 1 | 8.00 |
| CHEMBL3358116 | — | — | 1 | 7.96 |
| CHEMBL3358115 | — | — | 1 | 7.89 |
| CHEMBL3358126 | — | — | 1 | 7.89 |
| CHEMBL3357698 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3357685 | ZELENIRSTAT | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3357697 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3358121 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3358120 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3357699 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3358111 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3358114 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3358119 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3357682 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358122 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357693 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357695 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1230468 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357702 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358117 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358113 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358123 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3358125 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3357684 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3358127 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3358124 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3357703 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3357686 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3357700 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3358118 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3357706 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3358116 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3358115 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3358126 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3357698 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3358108 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3357688 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3357691 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3357687 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3357681 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3358110 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3357694 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3357704 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3357696 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3358112 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3358109 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3357683 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3357690 | — | EC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3357692 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3357705 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3357689 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3357701 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1951264 | — | EC50 | = | 16000.0 | nM | 4.80 |