Assay Detail
Functional
CHEMBL3129767
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay
38
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 8.07 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3127497 | — | — | 1 | 9.31 |
| CHEMBL3127507 | — | — | 1 | 9.31 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 9.00 |
| CHEMBL3127510 | — | — | 1 | 8.92 |
| CHEMBL3127493 | — | — | 1 | 8.74 |
| CHEMBL3127506 | — | — | 1 | 8.72 |
| CHEMBL3127501 | — | — | 1 | 8.72 |
| CHEMBL3127494 | — | — | 1 | 8.70 |
| CHEMBL3127500 | — | — | 1 | 8.55 |
| CHEMBL3127509 | — | — | 2 | 8.51 |
| CHEMBL3127508 | — | — | 1 | 8.51 |
| CHEMBL3127505 | — | — | 1 | 8.48 |
| CHEMBL3127504 | — | — | 1 | 8.36 |
| CHEMBL17289 | CHS-828 | 1.0 | 1 | 8.30 |
| CHEMBL3127521 | — | — | 1 | 8.24 |
| CHEMBL3127525 | — | — | 1 | 8.01 |
| CHEMBL3127511 | — | — | 1 | 7.96 |
| CHEMBL3127503 | — | — | 1 | 7.89 |
| CHEMBL3127520 | — | — | 2 | 7.89 |
| CHEMBL3127502 | — | — | 1 | 7.68 |
| CHEMBL3127499 | — | — | 1 | 7.66 |
| CHEMBL3127526 | — | — | 1 | 7.52 |
| CHEMBL3127524 | — | — | 1 | 7.28 |
| CHEMBL2393183 | — | — | 1 | 7.16 |
| CHEMBL3127498 | — | — | 1 | 6.92 |
| CHEMBL3127522 | — | — | 1 | 6.85 |
| CHEMBL3127514 | — | — | 1 | 6.10 |
| CHEMBL3127492 | — | — | 1 | - |
| CHEMBL3127515 | — | — | 1 | - |
| CHEMBL181 | DIAZOXIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3127507 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL3127497 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL566757 | DAPORINAD | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3127510 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3127493 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3127501 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3127506 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3127494 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3127500 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3127508 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3127509 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3127505 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3127504 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL17289 | CHS-828 | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3127521 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3127525 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3127511 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3127520 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3127503 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3127502 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3127499 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3127526 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3127524 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2393183 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3127498 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3127522 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL3127509 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3127514 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3127496 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127495 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127529 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127528 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127527 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127523 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127520 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127515 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3127492 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL181 | DIAZOXIDE | IC50 | - | — | - |