Assay Detail
Binding
CHEMBL5526697
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Inhibition of XPO1 in human Jurkat cells assessed as suppression of IL-2 expression incubated for 6 hrs by Bright-Glo Luciferase based microplate reader analysis
46
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Electrophile Determines Cellular Phenotypes among XPO1-Targeting Small Molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 46 | 7.01 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129857 | AS-602868 | 1.0 | 1 | 8.70 |
| CHEMBL5559223 | — | — | 1 | 8.40 |
| CHEMBL5555068 | — | — | 2 | 8.40 |
| CHEMBL5556912 | — | — | 1 | 8.40 |
| CHEMBL3898452 | — | — | 1 | 8.30 |
| CHEMBL5568605 | — | — | 1 | 8.15 |
| CHEMBL5542885 | — | — | 1 | 7.96 |
| CHEMBL3545185 | SELINEXOR | 4.0 | 1 | 7.92 |
| CHEMBL5566091 | — | — | 1 | 7.89 |
| CHEMBL5560534 | — | — | 1 | 7.72 |
| CHEMBL5564554 | — | — | 1 | 7.68 |
| CHEMBL5563530 | — | — | 1 | 7.64 |
| CHEMBL3545187 | VERDINEXOR | 2.0 | 1 | 7.62 |
| CHEMBL5562376 | — | — | 1 | 7.62 |
| CHEMBL5542505 | — | — | 1 | 7.60 |
| CHEMBL5542934 | — | — | 1 | 7.58 |
| CHEMBL5561373 | — | — | 1 | 7.40 |
| CHEMBL130837 | — | — | 1 | 7.32 |
| CHEMBL5556828 | — | — | 1 | 7.26 |
| CHEMBL5563179 | — | — | 1 | 7.24 |
| CHEMBL5562296 | — | — | 1 | 7.19 |
| CHEMBL130007 | — | — | 1 | 7.09 |
| CHEMBL5566432 | — | — | 1 | 7.08 |
| CHEMBL5564519 | — | — | 1 | 7.04 |
| CHEMBL336546 | — | — | 1 | 6.97 |
| CHEMBL5566341 | — | — | 1 | 6.86 |
| CHEMBL5555764 | — | — | 1 | 6.86 |
| CHEMBL5561263 | — | — | 1 | 6.84 |
| CHEMBL5560350 | — | — | 1 | 6.69 |
| CHEMBL5565311 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129857 | AS-602868 | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5559223 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5555068 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5556912 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3898452 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5555068 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5568605 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5542885 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3545185 | SELINEXOR | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5566091 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5560534 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5564554 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5563530 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3545187 | VERDINEXOR | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5562376 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5542505 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5542934 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5561373 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL130837 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5556828 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5563179 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5562296 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL130007 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5566432 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5564519 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL336546 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5566341 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5555764 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5561263 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL5560350 | — | EC50 | = | 206.0 | nM | 6.69 |
| CHEMBL5565311 | — | EC50 | = | 261.0 | nM | 6.58 |
| CHEMBL5567104 | — | EC50 | = | 358.0 | nM | 6.45 |
| CHEMBL5563366 | — | EC50 | = | 404.0 | nM | 6.39 |
| CHEMBL5567882 | — | EC50 | = | 501.0 | nM | 6.30 |
| CHEMBL5561442 | — | EC50 | = | 856.0 | nM | 6.07 |
| CHEMBL5562070 | — | EC50 | = | 913.0 | nM | 6.04 |
| CHEMBL5568216 | — | EC50 | = | 1334.0 | nM | 5.88 |
| CHEMBL5561311 | — | EC50 | = | 1396.0 | nM | 5.86 |
| CHEMBL424086 | — | EC50 | = | 1405.0 | nM | 5.85 |
| CHEMBL5563183 | — | EC50 | = | 1646.0 | nM | 5.78 |
| CHEMBL5561264 | — | EC50 | = | 2642.0 | nM | 5.58 |
| CHEMBL132495 | — | EC50 | = | 4090.0 | nM | 5.39 |
| CHEMBL5558576 | — | EC50 | = | 5406.0 | nM | 5.27 |
| CHEMBL5564418 | — | EC50 | = | 6690.0 | nM | 5.17 |
| CHEMBL5563692 | — | EC50 | = | 8123.0 | nM | 5.09 |
| CHEMBL5560389 | — | EC50 | > | 10000.0 | nM | - |