Assay Detail
Binding
CHEMBL3396926
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta(DE3) incubated for 15 mins prior to substrate addition measured after 30 mins
39
Total Activities
33
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
Nicotinamide phosphoribosyltransferase (CHEMBL1744525) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.56 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2420626 | — | — | 1 | 8.52 |
| CHEMBL3394727 | — | — | 1 | 8.30 |
| CHEMBL3394740 | — | — | 1 | 8.15 |
| CHEMBL3394741 | — | — | 1 | 8.10 |
| CHEMBL3394724 | — | — | 3 | 8.10 |
| CHEMBL3394730 | — | — | 1 | 8.00 |
| CHEMBL3394729 | — | — | 1 | 8.00 |
| CHEMBL3394734 | — | — | 1 | 8.00 |
| CHEMBL3394736 | — | — | 3 | 8.00 |
| CHEMBL2420620 | — | — | 1 | 8.00 |
| CHEMBL3394722 | — | — | 1 | 7.96 |
| CHEMBL3394728 | — | — | 1 | 7.96 |
| CHEMBL2420623 | — | — | 1 | 7.85 |
| CHEMBL2419504 | — | — | 1 | 7.82 |
| CHEMBL3394733 | — | — | 1 | 7.82 |
| CHEMBL3394725 | — | — | 1 | 7.72 |
| CHEMBL3394720 | — | — | 1 | 7.72 |
| CHEMBL3394721 | — | — | 1 | 7.72 |
| CHEMBL3394715 | — | — | 1 | 7.68 |
| CHEMBL3394723 | — | — | 3 | 7.58 |
| CHEMBL3394713 | — | — | 1 | 7.50 |
| CHEMBL3394737 | — | — | 1 | 7.47 |
| CHEMBL3394738 | — | — | 1 | 7.41 |
| CHEMBL3394735 | — | — | 1 | 7.41 |
| CHEMBL3394719 | — | — | 1 | 7.37 |
| CHEMBL3394716 | — | — | 1 | 7.33 |
| CHEMBL3394726 | — | — | 1 | 7.31 |
| CHEMBL3394718 | — | — | 1 | 7.15 |
| CHEMBL3394739 | — | — | 1 | 7.08 |
| CHEMBL3394714 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2420626 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3394727 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3394740 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3394741 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3394724 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2420620 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3394736 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3394734 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3394729 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3394730 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3394728 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3394722 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2420623 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3394733 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2419504 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3394720 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3394721 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3394725 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3394715 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3394724 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3394723 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3394713 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3394737 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3394736 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3394738 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3394735 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3394719 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3394716 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3394726 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3394723 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3394718 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3394739 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3394717 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3394714 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3394732 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3394731 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3394736 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3394724 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3394723 | — | IC50 | > | 2000.0 | nM | - |