Assay Detail
Binding
CHEMBL3271333
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Inhibition of C-terminal His-6-tagged full length human NAMPT expressed in Escherichia coli (DE3) cells after 30 mins by mass spectrometry-based analysis
29
Total Activities
29
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
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.17 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3260362 | — | — | 1 | 8.35 |
| CHEMBL2420629 | — | — | 1 | 8.30 |
| CHEMBL3260358 | — | — | 1 | 8.21 |
| CHEMBL3260359 | — | — | 1 | 8.11 |
| CHEMBL3260357 | — | — | 1 | 8.10 |
| CHEMBL3260364 | — | — | 1 | 8.09 |
| CHEMBL3260360 | — | — | 1 | 8.00 |
| CHEMBL3260366 | — | — | 1 | 8.00 |
| CHEMBL3260361 | — | — | 1 | 7.96 |
| CHEMBL3260363 | — | — | 1 | 7.92 |
| CHEMBL2420667 | — | — | 1 | 7.75 |
| CHEMBL2420666 | — | — | 1 | 7.55 |
| CHEMBL3260347 | — | — | 1 | 7.27 |
| CHEMBL3260367 | — | — | 1 | 7.00 |
| CHEMBL3260346 | — | — | 1 | 7.00 |
| CHEMBL3260356 | — | — | 1 | 6.96 |
| CHEMBL3260365 | — | — | 1 | 6.72 |
| CHEMBL3260353 | — | — | 1 | 6.52 |
| CHEMBL3260355 | — | — | 1 | 6.43 |
| CHEMBL3259825 | — | — | 1 | 6.41 |
| CHEMBL3260351 | — | — | 1 | 6.40 |
| CHEMBL3260350 | — | — | 1 | 6.39 |
| CHEMBL3260352 | — | — | 1 | 6.39 |
| CHEMBL3260354 | — | — | 1 | 6.36 |
| CHEMBL3260344 | — | — | 1 | 5.89 |
| CHEMBL3260348 | — | — | 1 | 5.77 |
| CHEMBL3260349 | — | — | 1 | 5.72 |
| CHEMBL3260343 | — | — | 1 | - |
| CHEMBL3260345 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3260362 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL2420629 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3260358 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3260359 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3260357 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3260364 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3260360 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3260366 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3260361 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3260363 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2420667 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2420666 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3260347 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3260367 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3260346 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3260356 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3260365 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3260353 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3260355 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3259825 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3260351 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3260350 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3260352 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3260354 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3260344 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3260348 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3260349 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3260343 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3260345 | — | IC50 | > | 2000.0 | nM | - |