Assay Detail
Functional
CHEMBL4388466
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutation assessed as inhibition of cell growth after 72 hrs by CCK-8 assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
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 | 7.38 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4579284 | — | — | 1 | 8.87 |
| CHEMBL4475995 | — | — | 1 | 8.65 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 8.32 |
| CHEMBL4578113 | — | — | 1 | 8.31 |
| CHEMBL4540043 | — | — | 1 | 8.20 |
| CHEMBL4453544 | — | — | 1 | 7.77 |
| CHEMBL4453985 | — | — | 1 | 7.60 |
| CHEMBL4522903 | — | — | 1 | 7.59 |
| CHEMBL4527968 | — | — | 1 | 7.48 |
| CHEMBL4454520 | — | — | 1 | 7.48 |
| CHEMBL4459869 | — | — | 1 | 7.39 |
| CHEMBL4562385 | — | — | 1 | 7.20 |
| CHEMBL4515592 | — | — | 1 | 6.84 |
| CHEMBL4561168 | — | — | 1 | 6.80 |
| CHEMBL4470144 | — | — | 1 | 6.76 |
| CHEMBL4451832 | — | — | 1 | 6.62 |
| CHEMBL4454348 | — | — | 1 | 6.58 |
| CHEMBL4518604 | — | — | 1 | 6.50 |
| CHEMBL4451262 | — | — | 1 | 6.48 |
| CHEMBL4516605 | — | — | 1 | 6.11 |
| CHEMBL4567362 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4579284 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL4475995 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL566757 | DAPORINAD | IC50 | = | 4.76 | nM | 8.32 |
| CHEMBL4578113 | — | IC50 | = | 4.88 | nM | 8.31 |
| CHEMBL4540043 | — | IC50 | = | 6.37 | nM | 8.20 |
| CHEMBL4453544 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL4453985 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4522903 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL4527968 | — | IC50 | = | 33.3 | nM | 7.48 |
| CHEMBL4454520 | — | IC50 | = | 33.4 | nM | 7.48 |
| CHEMBL4459869 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL4562385 | — | IC50 | = | 63.6 | nM | 7.20 |
| CHEMBL4515592 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4561168 | — | IC50 | = | 157.3 | nM | 6.80 |
| CHEMBL4470144 | — | IC50 | = | 174.6 | nM | 6.76 |
| CHEMBL4451832 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL4454348 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL4518604 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4451262 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4516605 | — | IC50 | = | 778.0 | nM | 6.11 |
| CHEMBL4567362 | — | IC50 | > | 10000.0 | nM | - |