Assay Detail
Binding
CHEMBL5363963
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST/His6-fused human full length GSK-3-beta (1 to 420 residues) expressed in Sf9 cells using RBERCHKtide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay
232
Total Activities
232
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 232 | 5.52 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5422486 | — | — | 1 | 7.03 |
| CHEMBL5441121 | — | — | 1 | 6.99 |
| CHEMBL5414801 | — | — | 1 | 6.92 |
| CHEMBL5438158 | — | — | 1 | 6.77 |
| CHEMBL5438293 | — | — | 1 | 6.70 |
| CHEMBL5416942 | — | — | 1 | 6.70 |
| CHEMBL5439276 | — | — | 1 | 6.64 |
| CHEMBL5405059 | — | — | 1 | 6.50 |
| CHEMBL5418722 | — | — | 1 | 6.44 |
| CHEMBL5429404 | — | — | 1 | 6.37 |
| CHEMBL5417147 | — | — | 1 | 6.34 |
| CHEMBL5409574 | — | — | 1 | 6.29 |
| CHEMBL1802358 | — | — | 1 | 6.22 |
| CHEMBL5438728 | — | — | 1 | 6.21 |
| CHEMBL5404544 | — | — | 1 | 6.19 |
| CHEMBL5417890 | — | — | 1 | 6.18 |
| CHEMBL5422654 | — | — | 1 | 6.18 |
| CHEMBL5434921 | — | — | 1 | 6.07 |
| CHEMBL5414514 | — | — | 1 | 6.07 |
| CHEMBL5400230 | — | — | 1 | 6.07 |
| CHEMBL5404644 | — | — | 1 | 6.02 |
| CHEMBL5397343 | — | — | 1 | 6.00 |
| CHEMBL5406081 | — | — | 1 | 5.95 |
| CHEMBL5407057 | — | — | 1 | 5.93 |
| CHEMBL5179655 | — | — | 1 | 5.92 |
| CHEMBL5414635 | — | — | 1 | 5.90 |
| CHEMBL5412565 | — | — | 1 | 5.88 |
| CHEMBL5396550 | — | — | 1 | 5.87 |
| CHEMBL5405680 | — | — | 1 | 5.87 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | 1.0 | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5422486 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5441121 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5414801 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5438158 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL5416942 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5438293 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL5439276 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL5405059 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL5418722 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL5429404 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL5417147 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL5409574 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL1802358 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5438728 | — | IC50 | = | 616.0 | nM | 6.21 |
| CHEMBL5404544 | — | IC50 | = | 647.0 | nM | 6.19 |
| CHEMBL5417890 | — | IC50 | = | 659.0 | nM | 6.18 |
| CHEMBL5422654 | — | IC50 | = | 663.0 | nM | 6.18 |
| CHEMBL5400230 | — | IC50 | = | 855.0 | nM | 6.07 |
| CHEMBL5414514 | — | IC50 | = | 847.0 | nM | 6.07 |
| CHEMBL5434921 | — | IC50 | = | 854.0 | nM | 6.07 |
| CHEMBL5404644 | — | IC50 | = | 947.0 | nM | 6.02 |
| CHEMBL5397343 | — | IC50 | = | 999.0 | nM | 6.00 |
| CHEMBL5406081 | — | IC50 | = | 1115.0 | nM | 5.95 |
| CHEMBL5407057 | — | IC50 | = | 1185.0 | nM | 5.93 |
| CHEMBL5179655 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5414635 | — | IC50 | = | 1267.0 | nM | 5.90 |
| CHEMBL5412565 | — | IC50 | = | 1334.0 | nM | 5.88 |
| CHEMBL5405680 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL5396550 | — | IC50 | = | 1359.0 | nM | 5.87 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | IC50 | = | 1461.0 | nM | 5.83 |
| CHEMBL5426735 | — | IC50 | = | 1559.0 | nM | 5.81 |
| CHEMBL5421200 | — | IC50 | = | 1552.0 | nM | 5.81 |
| CHEMBL5420645 | — | IC50 | = | 1541.0 | nM | 5.81 |
| CHEMBL5429783 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL5417527 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL5429707 | — | IC50 | = | 1738.0 | nM | 5.76 |
| CHEMBL5421442 | — | IC50 | = | 1798.0 | nM | 5.75 |
| CHEMBL5433644 | — | IC50 | = | 1831.0 | nM | 5.74 |
| CHEMBL5434349 | — | IC50 | = | 2155.0 | nM | 5.67 |
| CHEMBL5405969 | — | IC50 | = | 2147.0 | nM | 5.67 |
| CHEMBL5418020 | — | IC50 | = | 2225.0 | nM | 5.65 |
| CHEMBL5402979 | — | IC50 | = | 2414.0 | nM | 5.62 |
| CHEMBL5412101 | — | IC50 | = | 2437.0 | nM | 5.61 |
| CHEMBL5412105 | — | IC50 | = | 2519.0 | nM | 5.60 |
| CHEMBL5407529 | — | IC50 | = | 2577.0 | nM | 5.59 |
| CHEMBL5428132 | — | IC50 | = | 2604.0 | nM | 5.58 |
| CHEMBL5409730 | — | IC50 | = | 2685.0 | nM | 5.57 |
| CHEMBL5435490 | — | IC50 | = | 2743.0 | nM | 5.56 |
| CHEMBL5424272 | — | IC50 | = | 2771.0 | nM | 5.56 |
| CHEMBL5395707 | — | IC50 | = | 2839.0 | nM | 5.55 |