Assay Detail
Binding
CHEMBL2396492
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NAMPT (unknown origin) assessed as NAM conversion to NMN preincubated for 15 mins prior to substrate addition measured after 30 mins by mass spectrophotometric analysis
39
Total Activities
39
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 potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.45 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2393168 | — | — | 1 | 8.52 |
| CHEMBL2393183 | — | — | 1 | 8.52 |
| CHEMBL2391572 | — | — | 1 | 8.52 |
| CHEMBL2393173 | — | — | 1 | 8.40 |
| CHEMBL2393171 | — | — | 1 | 8.40 |
| CHEMBL2393190 | — | — | 1 | 8.40 |
| CHEMBL2393164 | — | — | 1 | 8.30 |
| CHEMBL2393163 | — | — | 1 | 8.22 |
| CHEMBL2393176 | — | — | 1 | 8.15 |
| CHEMBL2393172 | — | — | 1 | 8.10 |
| CHEMBL2393169 | — | — | 1 | 8.10 |
| CHEMBL2393158 | — | — | 1 | 8.00 |
| CHEMBL2393167 | — | — | 1 | 7.96 |
| CHEMBL2393178 | — | — | 1 | 7.92 |
| CHEMBL2393186 | — | — | 1 | 7.92 |
| CHEMBL2393182 | — | — | 1 | 7.89 |
| CHEMBL2393185 | — | — | 1 | 7.89 |
| CHEMBL2393189 | — | — | 1 | 7.85 |
| CHEMBL2393162 | — | — | 1 | 7.57 |
| CHEMBL2391567 | — | — | 1 | 7.55 |
| CHEMBL2393159 | — | — | 1 | 7.48 |
| CHEMBL2393177 | — | — | 1 | 7.40 |
| CHEMBL2393165 | — | — | 1 | 7.35 |
| CHEMBL2393160 | — | — | 1 | 7.33 |
| CHEMBL2393191 | — | — | 1 | 7.28 |
| CHEMBL2393174 | — | — | 1 | 7.23 |
| CHEMBL2393166 | — | — | 1 | 7.00 |
| CHEMBL2393161 | — | — | 1 | 6.99 |
| CHEMBL2393170 | — | — | 1 | 6.85 |
| CHEMBL2393192 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2393168 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2391572 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2393183 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2393173 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2393171 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2393190 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2393164 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2393163 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2393176 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2393172 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2393169 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2393158 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2393167 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2393178 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2393186 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2393182 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2393185 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2393189 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2393162 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2391567 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2393159 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2393177 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2393165 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2393160 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2393191 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2393174 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2393166 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2393161 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2393170 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL2393192 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL2393188 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2393181 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL2391551 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL2393187 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2393175 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2393179 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2393180 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2393193 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2393184 | — | IC50 | > | 2000.0 | nM | - |