Assay Detail
Binding
CHEMBL4416333
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged wild type human NNMT expressed in Escherichia coli NiCo21(DE3) assessed as reduction in 1-methylquinolinium level using quinoline as substrate in presence of SAM and measured every 27 seconds for 5.5 mins by fluorescence-based assay
36
Total Activities
35
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
High-Affinity Alkynyl Bisubstrate Inhibitors of Nicotinamide <i>N</i>-Methyltransferase (NNMT).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 6.89 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4553052 | — | — | 1 | 9.72 |
| CHEMBL4580446 | — | — | 1 | 9.62 |
| CHEMBL4591248 | — | — | 2 | 9.30 |
| CHEMBL4455627 | — | — | 1 | 8.73 |
| CHEMBL4449355 | — | — | 1 | 8.58 |
| CHEMBL4519184 | — | — | 1 | 8.47 |
| CHEMBL4435488 | — | — | 1 | 8.33 |
| CHEMBL4457046 | — | — | 1 | 8.30 |
| CHEMBL4473236 | — | — | 1 | 8.17 |
| CHEMBL4587553 | — | — | 1 | 8.05 |
| CHEMBL4565052 | — | — | 1 | 7.77 |
| CHEMBL4435314 | — | — | 1 | 7.49 |
| CHEMBL4584198 | — | — | 1 | 7.45 |
| CHEMBL4466178 | — | — | 1 | 7.26 |
| CHEMBL4554139 | — | — | 1 | 7.24 |
| CHEMBL4468322 | — | — | 1 | 7.12 |
| CHEMBL4067973 | — | — | 1 | 7.05 |
| CHEMBL4436433 | — | — | 1 | 6.97 |
| CHEMBL4435685 | — | — | 1 | 6.91 |
| CHEMBL4453138 | — | — | 1 | 6.71 |
| CHEMBL4515598 | — | — | 1 | 6.58 |
| CHEMBL4560891 | — | — | 1 | 6.36 |
| CHEMBL4100002 | — | — | 1 | 6.04 |
| CHEMBL4475449 | — | — | 1 | 5.98 |
| CHEMBL4536373 | — | — | 1 | 5.73 |
| CHEMBL4572786 | — | — | 1 | 5.43 |
| CHEMBL4544929 | — | — | 1 | 5.41 |
| CHEMBL4555136 | — | — | 1 | 5.24 |
| CHEMBL4520769 | — | — | 1 | 5.21 |
| CHEMBL4475113 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4553052 | — | Ki | = | 0.1905 | nM | 9.72 |
| CHEMBL4580446 | — | Ki | = | 0.2399 | nM | 9.62 |
| CHEMBL4591248 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4591248 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL4455627 | — | Ki | = | 1.862 | nM | 8.73 |
| CHEMBL4449355 | — | Ki | = | 2.63 | nM | 8.58 |
| CHEMBL4519184 | — | Ki | = | 3.388 | nM | 8.47 |
| CHEMBL4435488 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL4457046 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL4473236 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL4587553 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL4565052 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL4435314 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL4584198 | — | Ki | = | 35.48 | nM | 7.45 |
| CHEMBL4466178 | — | Ki | = | 54.95 | nM | 7.26 |
| CHEMBL4554139 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL4468322 | — | Ki | = | 75.86 | nM | 7.12 |
| CHEMBL4067973 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL4436433 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL4435685 | — | Ki | = | 123.03 | nM | 6.91 |
| CHEMBL4453138 | — | Ki | = | 194.98 | nM | 6.71 |
| CHEMBL4515598 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL4560891 | — | Ki | = | 436.52 | nM | 6.36 |
| CHEMBL4100002 | — | Ki | = | 912.01 | nM | 6.04 |
| CHEMBL4475449 | — | Ki | = | 1047.13 | nM | 5.98 |
| CHEMBL4536373 | — | Ki | = | 1862.09 | nM | 5.73 |
| CHEMBL4572786 | — | Ki | = | 3715.35 | nM | 5.43 |
| CHEMBL4544929 | — | Ki | = | 3890.45 | nM | 5.41 |
| CHEMBL4555136 | — | Ki | = | 5754.4 | nM | 5.24 |
| CHEMBL4520769 | — | Ki | = | 6165.95 | nM | 5.21 |
| CHEMBL4475113 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL4515831 | — | Ki | = | 19498.45 | nM | 4.71 |
| CHEMBL4434781 | — | Ki | = | 21379.62 | nM | 4.67 |
| CHEMBL4446074 | — | Ki | = | 22387.21 | nM | 4.65 |
| CHEMBL4466650 | — | Ki | = | 47863.01 | nM | 4.32 |
| CHEMBL4437201 | — | Ki | = | 77624.71 | nM | 4.11 |