Assay Detail
Binding
CHEMBL5734129
Review assay metadata, readout intent, target linkage, and publication context from the same page.
KinaseGlo Assay: PKR: Commercially available recombinant human GST-PKR (SignalChem, Canada; 1.5 uM-2 uM stock) is diluted to 500 nM in assay buffer (20 mM Tris-HCl, pH 7.2, 10 mM KCl, 10 mM MgCl2, 10% glycerol). Preactivated PKR is dispensed to 384/96-well black plates at 3.125/12.5 uls/well using the liquid handler Janus. Appropriate dilutions of inhibitors are added to 384/96-well plate followed by 6.6 uM ATP (final) and incubated for 10 minutes at room temperature. The remaining ATP/well is determined by adding 6.25/25 uls/well Kinase-Glo assay mix (Promega) and luminescence is measured on EnVision luminescence plate reader (integration time, 0.2 sec; Perkin-Elmer, Mass., USA). The % inhibition for the compounds is calculated using ATP only (100% inhibition) and PKR+ATP (0% inhibition).
36
Total Activities
12
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Interferon-induced, double-stranded RNA-activated protein kinase (CHEMBL5785) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Heterocycle-substituted pyridyl benzothiophenes as kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.84 | 7.41 |
| kon | 12 | - | - |
| k_off | 12 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5793168 | — | — | 3 | 7.41 |
| CHEMBL5995310 | — | — | 3 | 7.18 |
| CHEMBL5886368 | — | — | 3 | 7.12 |
| CHEMBL6062933 | — | — | 3 | 7.09 |
| CHEMBL5755281 | — | — | 3 | 7.00 |
| CHEMBL6041111 | — | — | 3 | 6.85 |
| CHEMBL5819668 | — | — | 3 | 6.80 |
| CHEMBL6063521 | — | — | 3 | 6.52 |
| CHEMBL5788618 | — | — | 3 | 6.25 |
| CHEMBL5996070 | — | — | 3 | 6.14 |
| CHEMBL5786084 | — | — | 3 | - |
| CHEMBL5779157 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5793168 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5995310 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5886368 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL6062933 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5755281 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL6041111 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5819668 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL6063521 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL5788618 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL5996070 | — | IC50 | = | 727.0 | nM | 6.14 |
| CHEMBL6062933 | — | kon | = | - | — | - |
| CHEMBL5996070 | — | kon | = | - | — | - |
| CHEMBL5995310 | — | k_off | = | - | s-1 | - |
| CHEMBL5995310 | — | kon | = | - | — | - |
| CHEMBL5886368 | — | k_off | = | - | s-1 | - |
| CHEMBL5886368 | — | kon | = | - | — | - |
| CHEMBL5755281 | — | k_off | = | - | s-1 | - |
| CHEMBL5755281 | — | kon | = | - | — | - |
| CHEMBL5793168 | — | k_off | = | - | s-1 | - |
| CHEMBL5793168 | — | kon | = | - | — | - |
| CHEMBL6041111 | — | k_off | = | - | s-1 | - |
| CHEMBL6041111 | — | kon | = | - | — | - |
| CHEMBL5996070 | — | k_off | = | - | s-1 | - |
| CHEMBL6062933 | — | k_off | = | - | s-1 | - |
| CHEMBL5786084 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL6063521 | — | kon | = | - | — | - |
| CHEMBL5788618 | — | k_off | = | - | s-1 | - |
| CHEMBL5788618 | — | kon | = | - | — | - |
| CHEMBL5779157 | — | k_off | = | - | s-1 | - |
| CHEMBL5779157 | — | kon | = | - | — | - |
| CHEMBL5779157 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5819668 | — | k_off | = | - | s-1 | - |
| CHEMBL5819668 | — | kon | = | - | — | - |
| CHEMBL5786084 | — | k_off | = | - | s-1 | - |
| CHEMBL6063521 | — | k_off | = | - | s-1 | - |
| CHEMBL5786084 | — | kon | = | - | — | - |