Assay Detail
Binding
CHEMBL5516166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IRE1alpha RNase activity (unknown origin) using XBP1 as substrate preincubated for 1 hr followed by thapsigargin stimulation for 5 hrs by One-Glo luciferase reagent based luminescence assay
33
Total Activities
33
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
Serine/threonine-protein kinase/endoribonuclease IRE1 (CHEMBL1163101) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.51 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5555999 | — | — | 1 | 7.75 |
| CHEMBL5562014 | — | — | 1 | 7.66 |
| CHEMBL5557276 | — | — | 1 | 7.51 |
| CHEMBL5557870 | — | — | 1 | 7.50 |
| CHEMBL5565861 | — | — | 1 | 7.50 |
| CHEMBL5558833 | — | — | 1 | 7.46 |
| CHEMBL5563969 | — | — | 1 | 7.43 |
| CHEMBL3356009 | — | — | 1 | 7.40 |
| CHEMBL5542252 | — | — | 1 | 7.38 |
| CHEMBL5561734 | — | — | 1 | 7.36 |
| CHEMBL5561325 | — | — | 1 | 7.33 |
| CHEMBL3356007 | — | — | 1 | 7.24 |
| CHEMBL5560090 | — | — | 1 | 7.08 |
| CHEMBL5555815 | — | — | 1 | 7.06 |
| CHEMBL5562143 | — | — | 1 | 6.85 |
| CHEMBL5532629 | — | — | 1 | 6.75 |
| CHEMBL5542651 | — | — | 1 | 6.70 |
| CHEMBL5555850 | — | — | 1 | 6.70 |
| CHEMBL5557507 | — | — | 1 | 6.52 |
| CHEMBL5556840 | — | — | 1 | 6.51 |
| CHEMBL5523599 | — | — | 1 | 6.48 |
| CHEMBL5532412 | — | — | 1 | 6.27 |
| CHEMBL5555363 | — | — | 1 | 5.89 |
| CHEMBL5560655 | — | — | 1 | 5.64 |
| CHEMBL5565839 | — | — | 1 | 5.64 |
| CHEMBL5567735 | — | — | 1 | 5.57 |
| CHEMBL5560044 | — | — | 1 | 5.36 |
| CHEMBL5560936 | — | — | 1 | 5.23 |
| CHEMBL5523348 | — | — | 1 | 5.05 |
| CHEMBL5561873 | — | — | 1 | 4.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5555999 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5562014 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5557276 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5557870 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5565861 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5558833 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5563969 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3356009 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5542252 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5561734 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5561325 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3356007 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5560090 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5555815 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5562143 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5532629 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5542651 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5555850 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5557507 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5556840 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5523599 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5532412 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5555363 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5560655 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5565839 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5567735 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5560044 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5560936 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL5523348 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL5561873 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL5558080 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL5565965 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL5557082 | — | IC50 | > | 50000.0 | nM | - |