Assay Detail
Binding
CHEMBL1954201
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Inhibition of human N-myristoyltransferase 1 using [3H]myristoyl-CoA and GCGGSKVKPQPPQAK(biotin)-amide as substrate preincubated for 5 mins prior substrate addition measured after 50 mins by streptavidin-coated scintillation proximity assay
27
Total Activities
27
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
Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.74 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230468 | — | — | 1 | 8.52 |
| CHEMBL1951295 | — | — | 1 | 8.15 |
| CHEMBL1951287 | — | — | 1 | 6.96 |
| CHEMBL1951296 | — | — | 1 | 6.92 |
| CHEMBL1951293 | — | — | 1 | 6.12 |
| CHEMBL1951282 | — | — | 1 | 6.00 |
| CHEMBL1951286 | — | — | 1 | 5.80 |
| CHEMBL1951284 | — | — | 1 | 5.62 |
| CHEMBL1951274 | — | — | 1 | 5.57 |
| CHEMBL1951291 | — | — | 1 | 5.38 |
| CHEMBL1951294 | — | — | 1 | 5.37 |
| CHEMBL1951277 | — | — | 1 | 5.09 |
| CHEMBL1951285 | — | — | 1 | 5.06 |
| CHEMBL1951278 | — | — | 1 | 4.80 |
| CHEMBL1951273 | — | — | 1 | 4.77 |
| CHEMBL1951105 | — | — | 1 | 4.66 |
| CHEMBL1951292 | — | — | 1 | 4.35 |
| CHEMBL1951279 | — | — | 1 | 4.13 |
| CHEMBL1951283 | — | — | 1 | - |
| CHEMBL1951288 | — | — | 1 | - |
| CHEMBL1951289 | — | — | 1 | - |
| CHEMBL1951290 | — | — | 1 | - |
| CHEMBL1951281 | — | — | 1 | - |
| CHEMBL1951280 | — | — | 1 | - |
| CHEMBL1951276 | — | — | 1 | - |
| CHEMBL1951275 | — | — | 1 | - |
| CHEMBL1951272 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230468 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1951295 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1951287 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1951296 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1951293 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1951282 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1951286 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1951284 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1951274 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1951291 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1951294 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1951277 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL1951285 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL1951278 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL1951273 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1951105 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL1951292 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL1951279 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL1951283 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1951288 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1951289 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1951290 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1951281 | — | IC50 | - | — | - | |
| CHEMBL1951280 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1951276 | — | IC50 | - | — | - | |
| CHEMBL1951275 | — | IC50 | - | — | - | |
| CHEMBL1951272 | — | IC50 | > | 100000.0 | nM | - |