Assay Detail
Binding
CHEMBL3096860
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nicotinamide phosphoribosyltransferase (CHEMBL1744525) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Nicotinamide phosphoribosyltransferase inhibitors, design, preparation, and structure-activity relationship.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.22 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3094250 | — | — | 1 | 9.70 |
| CHEMBL3094255 | — | — | 1 | 9.52 |
| CHEMBL3094249 | — | — | 1 | 8.96 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 8.66 |
| CHEMBL3094254 | — | — | 1 | 8.62 |
| CHEMBL3094258 | — | — | 1 | 8.62 |
| CHEMBL3094257 | — | — | 1 | 8.49 |
| CHEMBL3094229 | — | — | 1 | 8.44 |
| CHEMBL3094251 | — | — | 1 | 8.36 |
| CHEMBL3094236 | — | — | 1 | 8.09 |
| CHEMBL3094238 | — | — | 1 | 7.93 |
| CHEMBL17289 | CHS-828 | 1.0 | 1 | 7.74 |
| CHEMBL3094224 | — | — | 1 | 7.64 |
| CHEMBL2417795 | — | — | 1 | 7.42 |
| CHEMBL3094234 | — | — | 1 | 7.31 |
| CHEMBL3094230 | — | — | 1 | 7.30 |
| CHEMBL3094237 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3094250 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3094255 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3094249 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL566757 | DAPORINAD | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3094254 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3094258 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3094257 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3094229 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3094251 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3094236 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3094238 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL17289 | CHS-828 | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL3094224 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL2417795 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL3094234 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3094230 | — | IC50 | = | 49.6 | nM | 7.30 |
| CHEMBL3094237 | — | IC50 | = | 133.2 | nM | 6.88 |