Assay Detail
Binding
CHEMBL3238987
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Inhibition of Plasmodium falciparum N-myristoyltransferase by CPM fluorescence assay
33
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glycylpeptide N-tetradecanoyltransferase (CHEMBL2169722) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum (isolate 3D7) |
Publication
Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.90 | 8.10 |
| IC50 | 1 | 7.77 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237438 | — | — | 2 | 8.10 |
| CHEMBL3237425 | — | — | 1 | 7.82 |
| CHEMBL3237422 | — | — | 1 | 7.82 |
| CHEMBL3237412 | — | — | 1 | 7.58 |
| CHEMBL3237428 | — | — | 1 | 7.48 |
| CHEMBL3237424 | — | — | 1 | 7.30 |
| CHEMBL3237420 | — | — | 1 | 7.29 |
| CHEMBL3237436 | — | — | 1 | 7.26 |
| CHEMBL3237418 | — | — | 1 | 7.15 |
| CHEMBL3237427 | — | — | 1 | 7.11 |
| CHEMBL3237431 | — | — | 1 | 7.01 |
| CHEMBL3237437 | — | — | 1 | 6.95 |
| CHEMBL3237411 | — | — | 1 | 6.92 |
| CHEMBL3237423 | — | — | 1 | 6.92 |
| CHEMBL3237441 | — | — | 1 | 6.91 |
| CHEMBL3237435 | — | — | 1 | 6.90 |
| CHEMBL3237430 | — | — | 1 | 6.82 |
| CHEMBL3237421 | — | — | 1 | 6.79 |
| CHEMBL3237440 | — | — | 1 | 6.73 |
| CHEMBL3237434 | — | — | 1 | 6.67 |
| CHEMBL3237439 | — | — | 1 | 6.65 |
| CHEMBL3237419 | — | — | 1 | 6.61 |
| CHEMBL3237426 | — | — | 1 | 6.57 |
| CHEMBL3237429 | — | — | 1 | 6.48 |
| CHEMBL3237432 | — | — | 1 | 6.41 |
| CHEMBL3237433 | — | — | 1 | 6.33 |
| CHEMBL3237410 | — | — | 1 | 6.17 |
| CHEMBL3237414 | — | — | 1 | 5.95 |
| CHEMBL3237413 | — | — | 1 | 5.40 |
| CHEMBL3237415 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237438 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL3237425 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3237422 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3237438 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3237412 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3237428 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3237424 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3237420 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL3237436 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL3237418 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL3237427 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL3237431 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL3237437 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL3237411 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3237423 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3237441 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL3237435 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL3237430 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL3237421 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL3237440 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL3237434 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL3237439 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL3237419 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL3237426 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL3237429 | — | Ki | = | 334.0 | nM | 6.48 |
| CHEMBL3237432 | — | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL3237433 | — | Ki | = | 465.0 | nM | 6.33 |
| CHEMBL3237410 | — | Ki | = | 677.0 | nM | 6.17 |
| CHEMBL3237414 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL3237413 | — | Ki | = | 3970.0 | nM | 5.40 |
| CHEMBL3237415 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3237416 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3237417 | — | Ki | > | 10000.0 | nM | - |