Assay Detail
Binding
CHEMBL5735651
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Assay: Briefly, recombinant GSK3β kinase, ATP and Ser/Thr peptide 09 are prepared in 1× Kinase buffer to final concentrations of 0.04 μg/mL, 46 μM, and 4 μM respectively. The mixture is allowed to incubate with the representative compounds for one hour at room temperature. All reactions were performed in duplicate. Unphosphorylated (0% Control) and phosphorylated (100% control) forms of Ser/Thr 18 serve as control reactions.After incubation, diluted Development Buffer is added to the reaction and allowed to further incubate for one hour at room temperature. The plate is read at Ex 400 Em 455 to detect the coumarin signal and Ex 400 Em 520 to measure the signal (EnVision Multilabel Plate Reader, PerkinElmer).
210
Total Activities
66
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 |
Publication
6-(5-membered heteroaryl)isoquinolin-3-yl-(5-membered heteroaryl) carboxamides and preparation and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 70 | 5.85 | 8.05 |
| kon | 70 | - | - |
| k_off | 70 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5857120 | — | — | 3 | 8.05 |
| CHEMBL6000505 | — | — | 3 | 7.54 |
| CHEMBL5920679 | — | — | 3 | 6.64 |
| CHEMBL5995698 | — | — | 3 | 6.54 |
| CHEMBL5792391 | — | — | 3 | 6.53 |
| CHEMBL5783562 | — | — | 3 | 6.50 |
| CHEMBL5992147 | — | — | 3 | 6.49 |
| CHEMBL5854942 | — | — | 3 | 6.47 |
| CHEMBL4795948 | — | — | 3 | 6.46 |
| CHEMBL5989365 | — | — | 3 | 6.41 |
| CHEMBL6018003 | — | — | 3 | 6.40 |
| CHEMBL4800296 | — | — | 3 | 6.35 |
| CHEMBL5955685 | — | — | 3 | 6.34 |
| CHEMBL5996584 | — | — | 3 | 6.21 |
| CHEMBL6040830 | — | — | 3 | 6.20 |
| CHEMBL5994578 | — | — | 3 | 6.19 |
| CHEMBL5927873 | — | — | 3 | 6.18 |
| CHEMBL5873194 | — | — | 6 | 6.11 |
| CHEMBL6036161 | — | — | 3 | 6.11 |
| CHEMBL5782986 | — | — | 3 | 6.09 |
| CHEMBL5893883 | — | — | 3 | 6.07 |
| CHEMBL5752492 | — | — | 3 | 6.01 |
| CHEMBL6045084 | — | — | 6 | 5.98 |
| CHEMBL5940869 | — | — | 3 | 5.92 |
| CHEMBL5762477 | — | — | 3 | 5.90 |
| CHEMBL5886109 | — | — | 3 | 5.88 |
| CHEMBL5751532 | — | — | 3 | 5.88 |
| CHEMBL5892413 | — | — | 3 | 5.87 |
| CHEMBL4787749 | — | — | 3 | 5.85 |
| CHEMBL6015428 | — | — | 3 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5857120 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL6000505 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5920679 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5995698 | — | EC50 | = | 286.0 | nM | 6.54 |
| CHEMBL5792391 | — | EC50 | = | 295.0 | nM | 6.53 |
| CHEMBL5783562 | — | EC50 | = | 316.0 | nM | 6.50 |
| CHEMBL5992147 | — | EC50 | = | 322.0 | nM | 6.49 |
| CHEMBL5854942 | — | EC50 | = | 342.0 | nM | 6.47 |
| CHEMBL4795948 | — | EC50 | = | 349.0 | nM | 6.46 |
| CHEMBL5989365 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL6018003 | — | EC50 | = | 395.0 | nM | 6.40 |
| CHEMBL4800296 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5955685 | — | EC50 | = | 458.0 | nM | 6.34 |
| CHEMBL5996584 | — | EC50 | = | 611.0 | nM | 6.21 |
| CHEMBL6040830 | — | EC50 | = | 628.0 | nM | 6.20 |
| CHEMBL5994578 | — | EC50 | = | 641.0 | nM | 6.19 |
| CHEMBL5927873 | — | EC50 | = | 666.0 | nM | 6.18 |
| CHEMBL5873194 | — | EC50 | = | 769.0 | nM | 6.11 |
| CHEMBL6036161 | — | EC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5782986 | — | EC50 | = | 821.0 | nM | 6.09 |
| CHEMBL5893883 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL5873194 | — | EC50 | = | 979.0 | nM | 6.01 |
| CHEMBL5752492 | — | EC50 | = | 986.0 | nM | 6.01 |
| CHEMBL6045084 | — | EC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL5940869 | — | EC50 | = | 1194.0 | nM | 5.92 |
| CHEMBL5762477 | — | EC50 | = | 1263.0 | nM | 5.90 |
| CHEMBL5886109 | — | EC50 | = | 1335.0 | nM | 5.88 |
| CHEMBL5751532 | — | EC50 | = | 1326.0 | nM | 5.88 |
| CHEMBL5892413 | — | EC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4787749 | — | EC50 | = | 1415.0 | nM | 5.85 |
| CHEMBL4761662 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL6015428 | — | EC50 | = | 1495.0 | nM | 5.83 |
| CHEMBL6024982 | — | EC50 | = | 1614.0 | nM | 5.79 |
| CHEMBL6063563 | — | EC50 | = | 1656.0 | nM | 5.78 |
| CHEMBL6056650 | — | EC50 | = | 1655.0 | nM | 5.78 |
| CHEMBL5784059 | — | EC50 | = | 1704.0 | nM | 5.77 |
| CHEMBL4762838 | — | EC50 | = | 1755.0 | nM | 5.76 |
| CHEMBL5883539 | — | EC50 | = | 1769.0 | nM | 5.75 |
| CHEMBL6038529 | — | EC50 | = | 1826.0 | nM | 5.74 |
| CHEMBL5961069 | — | EC50 | = | 1921.0 | nM | 5.72 |
| CHEMBL4761662 | — | EC50 | = | 2063.0 | nM | 5.69 |
| CHEMBL5929615 | — | EC50 | = | 2082.0 | nM | 5.68 |
| CHEMBL6059586 | — | EC50 | = | 2189.0 | nM | 5.66 |
| CHEMBL5953637 | — | EC50 | = | 2179.0 | nM | 5.66 |
| CHEMBL6035523 | — | EC50 | = | 2339.0 | nM | 5.63 |
| CHEMBL4762553 | — | EC50 | = | 2586.0 | nM | 5.59 |
| CHEMBL5957402 | — | EC50 | = | 2747.0 | nM | 5.56 |
| CHEMBL6056931 | — | EC50 | = | 2934.0 | nM | 5.53 |
| CHEMBL5783383 | — | EC50 | = | 3058.0 | nM | 5.51 |
| CHEMBL4755579 | — | EC50 | = | 3071.0 | nM | 5.51 |