Assay Detail
Binding
CHEMBL3387684
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Inhibition of Trypanosoma brucei N-myristoyltransferase assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| IC50 | 48 | 8.24 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3357697 | — | — | 1 | 9.00 |
| CHEMBL3358127 | — | — | 1 | 8.70 |
| CHEMBL3358126 | — | — | 1 | 8.70 |
| CHEMBL3358125 | — | — | 1 | 8.70 |
| CHEMBL3358124 | — | — | 1 | 8.70 |
| CHEMBL3357685 | ZELENIRSTAT | 2.0 | 1 | 8.70 |
| CHEMBL3358123 | — | — | 1 | 8.70 |
| CHEMBL3358122 | — | — | 1 | 8.70 |
| CHEMBL3358121 | — | — | 1 | 8.70 |
| CHEMBL3357693 | — | — | 1 | 8.70 |
| CHEMBL3358114 | — | — | 1 | 8.70 |
| CHEMBL3357695 | — | — | 1 | 8.70 |
| CHEMBL3358113 | — | — | 1 | 8.70 |
| CHEMBL3358111 | — | — | 1 | 8.70 |
| CHEMBL3357702 | — | — | 1 | 8.70 |
| CHEMBL1230468 | — | — | 1 | 8.70 |
| CHEMBL3358120 | — | — | 1 | 8.70 |
| CHEMBL3358117 | — | — | 1 | 8.52 |
| CHEMBL3357699 | — | — | 1 | 8.52 |
| CHEMBL3357698 | — | — | 1 | 8.52 |
| CHEMBL3357691 | — | — | 1 | 8.52 |
| CHEMBL3357703 | — | — | 1 | 8.52 |
| CHEMBL3357706 | — | — | 1 | 8.52 |
| CHEMBL3358108 | — | — | 1 | 8.52 |
| CHEMBL3358110 | — | — | 1 | 8.52 |
| CHEMBL3358115 | — | — | 1 | 8.52 |
| CHEMBL3358118 | — | — | 1 | 8.52 |
| CHEMBL3358119 | — | — | 1 | 8.52 |
| CHEMBL3357682 | — | — | 1 | 8.40 |
| CHEMBL3358116 | — | — | 1 | 8.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3357697 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3358127 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358126 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358125 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358124 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357685 | ZELENIRSTAT | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358123 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358122 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358121 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358120 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357693 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358114 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357695 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358113 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3358111 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357702 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1230468 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357699 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3357698 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3357691 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3357703 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3357706 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358110 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358115 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358117 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358118 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358119 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3358108 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3357682 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3358116 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3357681 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3357700 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3357684 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3357687 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3357686 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3357694 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3357704 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3357696 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3357705 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3357688 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3358112 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3358109 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3357683 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3357692 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3357690 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3357701 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1951264 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3357689 | — | IC50 | = | 660.0 | nM | 6.18 |