Assay Detail
Binding
CHEMBL4388461
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant NAMPT (unknown origin) using NAM and PRPP as substrates incubated for 60 mins in presence of NMNAT1 measured at 5 mins interval for 30 mins by WST1 assay
21
Total Activities
21
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
Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.69 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4475995 | — | — | 1 | 8.29 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 8.17 |
| CHEMBL4579284 | — | — | 1 | 8.04 |
| CHEMBL4561168 | — | — | 1 | 8.02 |
| CHEMBL4453985 | — | — | 1 | 8.01 |
| CHEMBL4453544 | — | — | 1 | 8.01 |
| CHEMBL4540043 | — | — | 1 | 7.98 |
| CHEMBL4527968 | — | — | 1 | 7.97 |
| CHEMBL4578113 | — | — | 1 | 7.93 |
| CHEMBL4459869 | — | — | 1 | 7.91 |
| CHEMBL4522903 | — | — | 1 | 7.88 |
| CHEMBL4451832 | — | — | 1 | 7.84 |
| CHEMBL4451262 | — | — | 1 | 7.79 |
| CHEMBL4515592 | — | — | 1 | 7.78 |
| CHEMBL4562385 | — | — | 1 | 7.75 |
| CHEMBL4470144 | — | — | 1 | 7.61 |
| CHEMBL4516605 | — | — | 1 | 7.55 |
| CHEMBL4518604 | — | — | 1 | 7.50 |
| CHEMBL4454520 | — | — | 1 | 7.50 |
| CHEMBL4454348 | — | — | 1 | 6.63 |
| CHEMBL4567362 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4475995 | — | IC50 | = | 5.08 | nM | 8.29 |
| CHEMBL566757 | DAPORINAD | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4579284 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4561168 | — | IC50 | = | 9.47 | nM | 8.02 |
| CHEMBL4453985 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4453544 | — | IC50 | = | 9.78 | nM | 8.01 |
| CHEMBL4540043 | — | IC50 | = | 10.53 | nM | 7.98 |
| CHEMBL4527968 | — | IC50 | = | 10.75 | nM | 7.97 |
| CHEMBL4578113 | — | IC50 | = | 11.63 | nM | 7.93 |
| CHEMBL4459869 | — | IC50 | = | 12.28 | nM | 7.91 |
| CHEMBL4522903 | — | IC50 | = | 13.09 | nM | 7.88 |
| CHEMBL4451832 | — | IC50 | = | 14.42 | nM | 7.84 |
| CHEMBL4451262 | — | IC50 | = | 16.41 | nM | 7.79 |
| CHEMBL4515592 | — | IC50 | = | 16.54 | nM | 7.78 |
| CHEMBL4562385 | — | IC50 | = | 17.77 | nM | 7.75 |
| CHEMBL4470144 | — | IC50 | = | 24.53 | nM | 7.61 |
| CHEMBL4516605 | — | IC50 | = | 28.39 | nM | 7.55 |
| CHEMBL4518604 | — | IC50 | = | 31.32 | nM | 7.50 |
| CHEMBL4454520 | — | IC50 | = | 31.54 | nM | 7.50 |
| CHEMBL4454348 | — | IC50 | = | 234.5 | nM | 6.63 |
| CHEMBL4567362 | — | IC50 | = | 5920.0 | nM | 5.23 |