Assay Detail
Binding
CHEMBL5364218
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Binding affinity to full-length recombinant human NNMT expressed in Escherichia coli BL21(DE3) cells assessed as inhibition constant preincubated for 30 mins followed by FP probe addition measured after 30 mins by fluorescence polarization competition assay
28
Total Activities
28
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
Structure-Activity Relationship Studies on Cell-Potent Nicotinamide <i>N</i>-Methyltransferase Bisubstrate Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 6.04 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5408922 | — | — | 1 | 7.72 |
| CHEMBL5433732 | — | — | 1 | 7.42 |
| CHEMBL5407922 | — | — | 1 | 7.32 |
| CHEMBL5400606 | — | — | 1 | 7.31 |
| CHEMBL5437399 | — | — | 1 | 7.28 |
| CHEMBL5420435 | — | — | 1 | 7.14 |
| CHEMBL5403173 | — | — | 1 | 7.11 |
| CHEMBL5401131 | — | — | 1 | 7.02 |
| CHEMBL5432183 | — | — | 1 | 6.85 |
| CHEMBL5399278 | — | — | 1 | 6.72 |
| CHEMBL5432345 | — | — | 1 | 6.35 |
| CHEMBL5426689 | — | — | 1 | 6.19 |
| CHEMBL5417206 | — | — | 1 | 6.07 |
| CHEMBL5424430 | — | — | 1 | 5.85 |
| CHEMBL5409370 | — | — | 1 | 5.85 |
| CHEMBL5425170 | — | — | 1 | 5.68 |
| CHEMBL5434313 | — | — | 1 | 5.66 |
| CHEMBL5406466 | — | — | 1 | 5.55 |
| CHEMBL5411190 | — | — | 1 | 5.50 |
| CHEMBL5434023 | — | — | 1 | 5.39 |
| CHEMBL5404950 | — | — | 1 | 5.27 |
| CHEMBL5395424 | — | — | 1 | 5.00 |
| CHEMBL5395340 | — | — | 1 | 4.96 |
| CHEMBL5433740 | — | — | 1 | 4.92 |
| CHEMBL5429300 | — | — | 1 | 4.85 |
| CHEMBL5407102 | — | — | 1 | 4.77 |
| CHEMBL5414706 | — | — | 1 | 4.68 |
| CHEMBL5411538 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5408922 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL5433732 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL5407922 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL5400606 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL5437399 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL5420435 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL5403173 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL5401131 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL5432183 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL5399278 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL5432345 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL5426689 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL5417206 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL5424430 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL5409370 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL5425170 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL5434313 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL5406466 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL5411190 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL5434023 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL5404950 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL5395424 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL5395340 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL5433740 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL5429300 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL5407102 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL5414706 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL5411538 | — | Ki | = | 22000.0 | nM | 4.66 |