Assay Detail
Functional
CHEMBL3824713
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Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
39
Total Activities
39
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U-937 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 5.36 | 5.93 |
| GI50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3823107 | — | — | 1 | 5.93 |
| CHEMBL3823078 | — | — | 1 | 5.91 |
| CHEMBL3824326 | — | — | 1 | 5.85 |
| CHEMBL3822611 | — | — | 1 | 5.80 |
| CHEMBL3823031 | — | — | 1 | 5.78 |
| CHEMBL3397300 | — | — | 1 | 5.76 |
| CHEMBL3823235 | — | — | 1 | 5.75 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.64 |
| CHEMBL3823549 | — | — | 1 | 5.64 |
| CHEMBL3823268 | — | — | 1 | 5.63 |
| CHEMBL3823243 | — | — | 1 | 5.62 |
| CHEMBL3823218 | — | — | 1 | 5.57 |
| CHEMBL3822982 | — | — | 1 | 5.54 |
| CHEMBL3824130 | — | — | 1 | 5.53 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 5.50 |
| CHEMBL3824290 | — | — | 1 | 5.47 |
| CHEMBL3824308 | — | — | 1 | 5.46 |
| CHEMBL3823190 | — | — | 1 | 5.45 |
| CHEMBL3823916 | — | — | 1 | 5.34 |
| CHEMBL3824304 | — | — | 1 | 5.32 |
| CHEMBL3823256 | — | — | 1 | 5.32 |
| CHEMBL3824327 | — | — | 1 | 5.31 |
| CHEMBL3823577 | — | — | 1 | 5.28 |
| CHEMBL3824007 | — | — | 1 | 5.26 |
| CHEMBL3822557 | — | — | 1 | 5.25 |
| CHEMBL3823416 | — | — | 1 | 5.22 |
| CHEMBL3822645 | — | — | 1 | 5.21 |
| CHEMBL3823603 | — | — | 1 | 5.20 |
| CHEMBL3823872 | — | — | 1 | 5.16 |
| CHEMBL3823017 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3823107 | — | IC50 | = | 1174.0 | nM | 5.93 |
| CHEMBL3823078 | — | IC50 | = | 1231.0 | nM | 5.91 |
| CHEMBL3824326 | — | IC50 | = | 1423.0 | nM | 5.85 |
| CHEMBL3822611 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL3823031 | — | IC50 | = | 1678.0 | nM | 5.78 |
| CHEMBL3397300 | — | IC50 | = | 1718.0 | nM | 5.76 |
| CHEMBL3823235 | — | IC50 | = | 1798.0 | nM | 5.75 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 2286.0 | nM | 5.64 |
| CHEMBL3823549 | — | IC50 | = | 2307.0 | nM | 5.64 |
| CHEMBL3823268 | — | IC50 | = | 2368.0 | nM | 5.63 |
| CHEMBL3823243 | — | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL3823218 | — | IC50 | = | 2725.0 | nM | 5.57 |
| CHEMBL3822982 | — | IC50 | = | 2908.0 | nM | 5.54 |
| CHEMBL3824130 | — | IC50 | = | 2968.0 | nM | 5.53 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 3194.0 | nM | 5.50 |
| CHEMBL3824290 | — | IC50 | = | 3389.0 | nM | 5.47 |
| CHEMBL3824308 | — | IC50 | = | 3465.0 | nM | 5.46 |
| CHEMBL3823190 | — | IC50 | = | 3557.0 | nM | 5.45 |
| CHEMBL3823916 | — | IC50 | = | 4523.0 | nM | 5.34 |
| CHEMBL3824304 | — | IC50 | = | 4838.0 | nM | 5.32 |
| CHEMBL3823256 | — | IC50 | = | 4813.0 | nM | 5.32 |
| CHEMBL3824327 | — | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL3823577 | — | IC50 | = | 5307.0 | nM | 5.28 |
| CHEMBL3824007 | — | IC50 | = | 5453.0 | nM | 5.26 |
| CHEMBL3822557 | — | IC50 | = | 5682.0 | nM | 5.25 |
| CHEMBL3823416 | — | IC50 | = | 5994.0 | nM | 5.22 |
| CHEMBL3822645 | — | IC50 | = | 6226.0 | nM | 5.21 |
| CHEMBL3823603 | — | IC50 | = | 6334.0 | nM | 5.20 |
| CHEMBL3823872 | — | IC50 | = | 7004.0 | nM | 5.16 |
| CHEMBL3823017 | — | IC50 | = | 7232.0 | nM | 5.14 |
| CHEMBL3822524 | — | IC50 | = | 10630.0 | nM | 4.97 |
| CHEMBL3823165 | — | IC50 | = | 13193.0 | nM | 4.88 |
| CHEMBL3823198 | — | IC50 | = | 13863.0 | nM | 4.86 |
| CHEMBL3822973 | — | IC50 | = | 20824.0 | nM | 4.68 |
| CHEMBL3823224 | — | IC50 | = | 21475.0 | nM | 4.67 |
| CHEMBL3824318 | — | IC50 | = | 22398.0 | nM | 4.65 |
| CHEMBL3823296 | — | IC50 | = | 24166.0 | nM | 4.62 |
| CHEMBL3822589 | — | IC50 | - | — | - | |
| CHEMBL3823836 | — | GI50 | = | 1282.0 | nM | - |