Assay Detail
Binding
CHEMBL3387685
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-myristoyltransferase 1 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 | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glycylpeptide N-tetradecanoyltransferase 1 (CHEMBL2593) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.25 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230468 | — | — | 1 | 8.52 |
| CHEMBL3357697 | — | — | 1 | 8.40 |
| CHEMBL3357685 | ZELENIRSTAT | 2.0 | 1 | 8.40 |
| CHEMBL3358119 | — | — | 1 | 8.40 |
| CHEMBL3357702 | — | — | 1 | 8.40 |
| CHEMBL3357699 | — | — | 1 | 8.30 |
| CHEMBL3358121 | — | — | 1 | 8.30 |
| CHEMBL3358120 | — | — | 1 | 8.30 |
| CHEMBL3358122 | — | — | 1 | 8.10 |
| CHEMBL3357695 | — | — | 1 | 8.10 |
| CHEMBL3358117 | — | — | 1 | 8.05 |
| CHEMBL3357704 | — | — | 1 | 8.05 |
| CHEMBL3357681 | — | — | 1 | 8.05 |
| CHEMBL3358114 | — | — | 1 | 7.92 |
| CHEMBL3357682 | — | — | 1 | 7.92 |
| CHEMBL3357705 | — | — | 1 | 7.77 |
| CHEMBL3357686 | — | — | 1 | 7.77 |
| CHEMBL3358111 | — | — | 1 | 7.75 |
| CHEMBL3357703 | — | — | 1 | 7.66 |
| CHEMBL3357687 | — | — | 1 | 7.64 |
| CHEMBL3358113 | — | — | 1 | 7.62 |
| CHEMBL3357684 | — | — | 1 | 7.60 |
| CHEMBL3357688 | — | — | 1 | 7.60 |
| CHEMBL3357700 | — | — | 1 | 7.54 |
| CHEMBL3357693 | — | — | 1 | 7.48 |
| CHEMBL3357698 | — | — | 1 | 7.40 |
| CHEMBL3358125 | — | — | 1 | 7.35 |
| CHEMBL3358127 | — | — | 1 | 7.33 |
| CHEMBL3357683 | — | — | 1 | 7.23 |
| CHEMBL3358123 | — | — | 1 | 7.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230468 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3357697 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3357702 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3357685 | ZELENIRSTAT | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3358119 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3357699 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3358121 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3358120 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3358122 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3357695 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3358117 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3357704 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3357681 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3357682 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3358114 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3357705 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3357686 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3358111 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3357703 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3357687 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3358113 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3357684 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3357688 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3357700 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3357693 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3357698 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3358125 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3358127 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3357683 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3358123 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3357696 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3358126 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3358118 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3358115 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3357706 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3357694 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3358116 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3358124 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3358110 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3358108 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3357691 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3358112 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3358109 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3357692 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3357701 | — | IC50 | = | 3580.0 | nM | 5.45 |
| CHEMBL3357690 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1951264 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL3357689 | — | IC50 | = | 17000.0 | nM | 4.77 |