Assay Detail
Binding
CHEMBL4036655
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His-tagged human recombinant NAMPT using FK866 or isoindoline urea-based Oregon green (488) probe incubated for 3 hrs by TR-FRET assay
47
Total Activities
47
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
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 47 | 7.84 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3943749 | — | — | 1 | 9.00 |
| CHEMBL4060799 | — | — | 1 | 8.82 |
| CHEMBL3960317 | — | — | 1 | 8.80 |
| CHEMBL4083505 | — | — | 1 | 8.77 |
| CHEMBL4096471 | — | — | 1 | 8.72 |
| CHEMBL4089003 | — | — | 1 | 8.60 |
| CHEMBL17289 | CHS-828 | 1.0 | 1 | 8.52 |
| CHEMBL3922276 | — | — | 1 | 8.52 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 8.52 |
| CHEMBL4076064 | — | — | 1 | 8.41 |
| CHEMBL4105475 | — | — | 1 | 8.37 |
| CHEMBL3972460 | — | — | 1 | 8.33 |
| CHEMBL3913732 | — | — | 1 | 8.31 |
| CHEMBL4086819 | — | — | 1 | 8.29 |
| CHEMBL3984857 | — | — | 1 | 8.27 |
| CHEMBL4082366 | — | — | 1 | 8.25 |
| CHEMBL3908312 | — | — | 1 | 8.12 |
| CHEMBL3926822 | — | — | 1 | 8.10 |
| CHEMBL3938019 | — | — | 1 | 8.05 |
| CHEMBL4077485 | — | — | 1 | 8.03 |
| CHEMBL3950120 | — | — | 1 | 7.96 |
| CHEMBL3904786 | — | — | 1 | 7.89 |
| CHEMBL3941284 | — | — | 1 | 7.89 |
| CHEMBL3892230 | — | — | 1 | 7.85 |
| CHEMBL4062838 | — | — | 1 | 7.85 |
| CHEMBL3896390 | — | — | 1 | 7.82 |
| CHEMBL3925932 | — | — | 1 | 7.80 |
| CHEMBL3953911 | — | — | 1 | 7.77 |
| CHEMBL3975643 | — | — | 1 | 7.75 |
| CHEMBL3930840 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3943749 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4060799 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3960317 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4083505 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4096471 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL4089003 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL17289 | CHS-828 | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3922276 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL566757 | DAPORINAD | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4076064 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4105475 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL3972460 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL3913732 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL4086819 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL3984857 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL4082366 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL3908312 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL3926822 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3938019 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4077485 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL3950120 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3904786 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3941284 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3892230 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4062838 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3896390 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3925932 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3953911 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3975643 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3930840 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3899179 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3907814 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4076641 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3890168 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3940058 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3974537 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4077254 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3918436 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL3937583 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL4081887 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL4099778 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3949149 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL2419508 | — | Ki | = | 487.0 | nM | 6.31 |
| CHEMBL3890237 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL3715249 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4090863 | — | Ki | > | 8900.0 | nM | - |
| CHEMBL4062656 | — | Ki | > | 9000.0 | nM | - |