Assay Detail
Binding
CHEMBL4810079
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Inhibition of human recombinant NNMT using nicotinamide and SAM as substrate assessed as reduction in 1-methyl-nicotinamide formation incubated for 22 to 24 hrs by RapidFire Mass spectroscopy
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 |
Publication
Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.56 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4867273 | — | — | 1 | 9.82 |
| CHEMBL4859806 | — | — | 1 | 9.40 |
| CHEMBL4847740 | — | — | 1 | 9.33 |
| CHEMBL4857394 | — | — | 1 | 9.03 |
| CHEMBL4878738 | — | — | 1 | 8.96 |
| CHEMBL4872872 | — | — | 1 | 8.72 |
| CHEMBL4856854 | — | — | 1 | 8.24 |
| CHEMBL4848464 | — | — | 1 | 7.85 |
| CHEMBL4853328 | — | — | 1 | 7.85 |
| CHEMBL4868588 | — | — | 1 | 7.55 |
| CHEMBL4859039 | — | — | 1 | 7.44 |
| CHEMBL4849636 | — | — | 1 | 7.38 |
| CHEMBL4858283 | — | — | 1 | 7.35 |
| CHEMBL4868364 | — | — | 1 | 7.28 |
| CHEMBL4863816 | — | — | 1 | 7.21 |
| CHEMBL4875414 | — | — | 1 | 6.97 |
| CHEMBL4870987 | — | — | 1 | 6.90 |
| CHEMBL4860372 | — | — | 1 | 6.85 |
| CHEMBL4873940 | — | — | 1 | 6.84 |
| CHEMBL4878905 | — | — | 1 | 6.67 |
| CHEMBL4851654 | — | — | 1 | 6.66 |
| CHEMBL4856886 | — | — | 1 | 6.19 |
| CHEMBL4868547 | — | — | 1 | 5.57 |
| CHEMBL4869822 | — | — | 1 | 5.38 |
| CHEMBL4856096 | — | — | 1 | - |
| CHEMBL4875995 | — | — | 1 | - |
| CHEMBL4859787 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4867273 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4859806 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4847740 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL4857394 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL4878738 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4872872 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4856854 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4848464 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4853328 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4868588 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4859039 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4849636 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4858283 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4868364 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4863816 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4875414 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4870987 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4860372 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4873940 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4878905 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4851654 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL4856886 | — | IC50 | = | 648.0 | nM | 6.19 |
| CHEMBL4868547 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4869822 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL4856096 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4875995 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4859787 | — | IC50 | > | 30000.0 | nM | - |