Assay Detail
Binding
CHEMBL5735170
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Assay : The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologiesa Division of Thermo-Fisher). This is a non-radioactive assay using fluorescence resonance energy transfer (FRET) between coumarin and fluorescein to detect kinase activity which is represented as ratio of coumarin emission/fluorescein emission.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.
453
Total Activities
143
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-(6-membered heteroaryl and aryl)isoquinolin-3-yl carboxamides and preparation and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 151 | 6.23 | 8.52 |
| kon | 151 | - | - |
| k_off | 151 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4777070 | — | — | 3 | 8.52 |
| CHEMBL5960963 | — | — | 3 | 8.40 |
| CHEMBL6062643 | — | — | 3 | 8.00 |
| CHEMBL5829160 | — | — | 3 | 7.89 |
| CHEMBL4751376 | — | — | 3 | 7.85 |
| CHEMBL5930315 | — | — | 3 | 7.77 |
| CHEMBL5975278 | — | — | 3 | 7.58 |
| CHEMBL5835564 | — | — | 3 | 7.51 |
| CHEMBL5750669 | — | — | 3 | 7.42 |
| CHEMBL5962131 | — | — | 3 | 7.32 |
| CHEMBL4761487 | — | — | 3 | 7.30 |
| CHEMBL6036201 | — | — | 3 | 7.25 |
| CHEMBL5868738 | — | — | 3 | 7.25 |
| CHEMBL5869786 | — | — | 3 | 7.24 |
| CHEMBL5923924 | — | — | 3 | 7.17 |
| CHEMBL5937460 | — | — | 3 | 7.17 |
| CHEMBL6017939 | — | — | 3 | 7.11 |
| CHEMBL6036676 | — | — | 3 | 7.04 |
| CHEMBL5784549 | — | — | 3 | 7.01 |
| CHEMBL5985416 | — | — | 3 | 6.96 |
| CHEMBL5973337 | — | — | 3 | 6.89 |
| CHEMBL5908483 | — | — | 3 | 6.76 |
| CHEMBL5915631 | — | — | 6 | 6.76 |
| CHEMBL5904897 | — | — | 3 | 6.75 |
| CHEMBL5761359 | — | — | 3 | 6.75 |
| CHEMBL4763112 | — | — | 3 | 6.71 |
| CHEMBL5897511 | — | — | 6 | 6.61 |
| CHEMBL6000795 | — | — | 3 | 6.59 |
| CHEMBL5942453 | — | — | 3 | 6.58 |
| CHEMBL5869074 | — | — | 3 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4777070 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5960963 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6062643 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5829160 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4751376 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5930315 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5975278 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5835564 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5750669 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5962131 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4761487 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5868738 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL6036201 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5869786 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5923924 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5937460 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL6017939 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL6036676 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5784549 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5985416 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5973337 | — | EC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5908483 | — | EC50 | = | 175.0 | nM | 6.76 |
| CHEMBL5915631 | — | EC50 | = | 175.0 | nM | 6.76 |
| CHEMBL5761359 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5904897 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4763112 | — | EC50 | = | 193.0 | nM | 6.71 |
| CHEMBL5897511 | — | EC50 | = | 247.0 | nM | 6.61 |
| CHEMBL6000795 | — | EC50 | = | 256.0 | nM | 6.59 |
| CHEMBL5942453 | — | EC50 | = | 264.0 | nM | 6.58 |
| CHEMBL5869074 | — | EC50 | = | 283.0 | nM | 6.55 |
| CHEMBL5897511 | — | EC50 | = | 404.0 | nM | 6.39 |
| CHEMBL5984644 | — | EC50 | = | 455.0 | nM | 6.34 |
| CHEMBL5868573 | — | EC50 | = | 487.0 | nM | 6.31 |
| CHEMBL5984644 | — | EC50 | = | 525.0 | nM | 6.28 |
| CHEMBL5860875 | — | EC50 | = | 602.0 | nM | 6.22 |
| CHEMBL5915631 | — | EC50 | = | 609.0 | nM | 6.21 |
| CHEMBL5914776 | — | EC50 | = | 623.0 | nM | 6.21 |
| CHEMBL5812391 | — | EC50 | = | 652.0 | nM | 6.19 |
| CHEMBL6019076 | — | EC50 | = | 698.0 | nM | 6.16 |
| CHEMBL5802614 | — | EC50 | = | 725.0 | nM | 6.14 |
| CHEMBL6056579 | — | EC50 | = | 722.0 | nM | 6.14 |
| CHEMBL5836134 | — | EC50 | = | 748.0 | nM | 6.13 |
| CHEMBL5851800 | — | EC50 | = | 755.0 | nM | 6.12 |
| CHEMBL5984644 | — | EC50 | = | 795.0 | nM | 6.10 |
| CHEMBL5977519 | — | EC50 | = | 804.0 | nM | 6.09 |
| CHEMBL5769881 | — | EC50 | = | 828.0 | nM | 6.08 |
| CHEMBL5740373 | — | EC50 | = | 859.0 | nM | 6.07 |
| CHEMBL5797249 | — | EC50 | = | 957.0 | nM | 6.02 |
| CHEMBL5928049 | — | EC50 | = | 974.0 | nM | 6.01 |
| CHEMBL5888317 | — | EC50 | = | 1026.0 | nM | 5.99 |