Assay Detail
Binding
CHEMBL3867189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins in presence of PRPP
69
Total Activities
69
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
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 69 | 7.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2417572 | — | — | 1 | 8.70 |
| CHEMBL17289 | CHS-828 | 1.0 | 1 | 8.70 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 8.52 |
| CHEMBL2391572 | — | — | 1 | 8.52 |
| CHEMBL2393183 | — | — | 1 | 8.52 |
| CHEMBL3127521 | — | — | 1 | 8.40 |
| CHEMBL3958233 | — | — | 1 | 8.36 |
| CHEMBL2420629 | — | — | 1 | 8.30 |
| CHEMBL3916438 | — | — | 1 | 8.26 |
| CHEMBL3260358 | — | — | 1 | 8.22 |
| CHEMBL3968268 | — | — | 1 | 8.22 |
| CHEMBL2393163 | — | — | 1 | 8.22 |
| CHEMBL3914526 | — | — | 1 | 8.21 |
| CHEMBL3913883 | — | — | 1 | 8.17 |
| CHEMBL3893879 | — | — | 1 | 8.15 |
| CHEMBL2391568 | — | — | 1 | 8.15 |
| CHEMBL2420620 | — | — | 1 | 8.10 |
| CHEMBL3949594 | — | — | 1 | 8.07 |
| CHEMBL3902837 | — | — | 1 | 8.05 |
| CHEMBL3897803 | — | — | 1 | 8.00 |
| CHEMBL3921880 | — | — | 1 | 8.00 |
| CHEMBL3394734 | — | — | 1 | 8.00 |
| CHEMBL2419515 | — | — | 1 | 7.96 |
| CHEMBL3986197 | — | — | 1 | 7.92 |
| CHEMBL3925878 | — | — | 1 | 7.89 |
| CHEMBL3948584 | — | — | 1 | 7.89 |
| CHEMBL3907541 | — | — | 1 | 7.85 |
| CHEMBL3923552 | — | — | 1 | 7.85 |
| CHEMBL2419505 | — | — | 1 | 7.85 |
| CHEMBL3939767 | — | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2417572 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL17289 | CHS-828 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2391572 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2393183 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL566757 | DAPORINAD | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3127521 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3958233 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL2420629 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3916438 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3260358 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3968268 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2393163 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3914526 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3913883 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL2391568 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3893879 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2420620 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3949594 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3902837 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3897803 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3921880 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3394734 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2419515 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3986197 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL3948584 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3925878 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL3907541 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3923552 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2419505 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3939767 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL2419504 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3889487 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL3983716 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL3930818 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3974268 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL3984355 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3908644 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3963163 | — | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL3904503 | — | IC50 | = | 21.9 | nM | 7.66 |
| CHEMBL3948512 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL3972073 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3941475 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL3940454 | — | IC50 | = | 27.4 | nM | 7.56 |
| CHEMBL3920776 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3977721 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL3394738 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3895553 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3921809 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL3930755 | — | IC50 | = | 48.1 | nM | 7.32 |
| CHEMBL3913503 | — | IC50 | = | 47.8 | nM | 7.32 |