Assay Detail
Binding
CHEMBL4673066
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Inhibition of IRE1alpha (unknown origin) assessed as XBP-1 slicing luciferase activity incubated for 1 hr followed by stimulation with thapsigargin measured after 5 hrs by luciferase reporter gene assay
22
Total Activities
22
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
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.82 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4752754 | — | — | 1 | 7.36 |
| CHEMBL4758147 | — | — | 1 | 7.32 |
| CHEMBL3356007 | — | — | 1 | 7.24 |
| CHEMBL4781285 | — | — | 1 | 6.92 |
| CHEMBL4754759 | — | — | 1 | 6.82 |
| CHEMBL4747176 | — | — | 1 | 6.55 |
| CHEMBL4786638 | — | — | 1 | 6.50 |
| CHEMBL4760343 | — | — | 1 | 6.41 |
| CHEMBL4757144 | — | — | 1 | 5.96 |
| CHEMBL4758021 | — | — | 1 | 5.80 |
| CHEMBL4743690 | — | — | 1 | 5.77 |
| CHEMBL4759829 | — | — | 1 | 5.70 |
| CHEMBL4787548 | — | — | 1 | 5.50 |
| CHEMBL4755886 | — | — | 1 | 5.31 |
| CHEMBL4749470 | — | — | 1 | 5.28 |
| CHEMBL4780489 | — | — | 1 | 5.25 |
| CHEMBL4759055 | — | — | 1 | 5.00 |
| CHEMBL4753548 | — | — | 1 | 4.90 |
| CHEMBL4753081 | — | — | 1 | 4.72 |
| CHEMBL4749836 | — | — | 1 | 4.72 |
| CHEMBL4744569 | — | — | 1 | 4.54 |
| CHEMBL4740654 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4752754 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4758147 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3356007 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4781285 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4754759 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4747176 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4786638 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4760343 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4757144 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4758021 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4743690 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4759829 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4787548 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4755886 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4749470 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4780489 | — | IC50 | = | 5580.0 | nM | 5.25 |
| CHEMBL4759055 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4753548 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4753081 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4749836 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4744569 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL4740654 | — | IC50 | = | 31000.0 | nM | 4.51 |