Assay Detail
Binding
CHEMBL4673064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged IRE1alpha D688N mutant KR domain (G547 to L997 reidues) (unknown origin) expressed in Sf9 insect cells measured after 1 hr by fluorescent labeled probe based TR-FRET assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.99 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4758021 | — | — | 1 | 8.48 |
| CHEMBL3356007 | — | — | 1 | 8.43 |
| CHEMBL4755886 | — | — | 1 | 8.43 |
| CHEMBL4760343 | — | — | 1 | 8.41 |
| CHEMBL4781285 | — | — | 1 | 8.36 |
| CHEMBL4754759 | — | — | 1 | 8.31 |
| CHEMBL4757144 | — | — | 1 | 8.30 |
| CHEMBL4759829 | — | — | 1 | 8.29 |
| CHEMBL4786638 | — | — | 1 | 8.29 |
| CHEMBL4747176 | — | — | 1 | 8.28 |
| CHEMBL4752754 | — | — | 1 | 8.28 |
| CHEMBL4749470 | — | — | 1 | 8.27 |
| CHEMBL4787548 | — | — | 1 | 8.26 |
| CHEMBL4780489 | — | — | 1 | 8.17 |
| CHEMBL4758147 | — | — | 1 | 8.15 |
| CHEMBL4743690 | — | — | 1 | 8.11 |
| CHEMBL4753548 | — | — | 1 | 8.05 |
| CHEMBL4753081 | — | — | 1 | 7.68 |
| CHEMBL4740654 | — | — | 1 | 7.24 |
| CHEMBL4759055 | — | — | 1 | 6.85 |
| CHEMBL4749836 | — | — | 1 | 6.68 |
| CHEMBL4744569 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4758021 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3356007 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4755886 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4760343 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4781285 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4754759 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4757144 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4759829 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4786638 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4747176 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4752754 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4749470 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4787548 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4780489 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4758147 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4743690 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4753548 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4753081 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4740654 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4759055 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4749836 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4744569 | — | IC50 | = | 400.0 | nM | 6.40 |