Assay Detail
Binding
CHEMBL5251385
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human GSK-3beta assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 37 | 6.64 | 10.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4647659 | — | — | 1 | 10.34 |
| CHEMBL1997924 | — | — | 1 | 8.71 |
| CHEMBL5285332 | — | — | 1 | 8.43 |
| CHEMBL393525 | — | — | 1 | 8.40 |
| CHEMBL5289681 | — | — | 1 | 8.21 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.12 |
| CHEMBL4297639 | LORECIVIVINT | 3.0 | 1 | 6.81 |
| CHEMBL3894571 | — | — | 1 | 6.80 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 6.67 |
| CHEMBL4873449 | — | — | 1 | 6.58 |
| CHEMBL5279705 | — | — | 1 | 6.40 |
| CHEMBL3589662 | — | — | 1 | 6.32 |
| CHEMBL1802358 | — | — | 1 | 6.25 |
| CHEMBL5081787 | — | — | 1 | 6.03 |
| CHEMBL5086263 | — | — | 1 | 6.03 |
| CHEMBL4784318 | CIRTUVIVINT | 1.0 | 1 | 5.93 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 5.89 |
| CHEMBL1232500 | — | — | 1 | 5.78 |
| CHEMBL5091238 | — | — | 1 | 5.75 |
| CHEMBL3298236 | — | — | 1 | 5.70 |
| CHEMBL5283849 | — | — | 1 | 5.60 |
| CHEMBL4283240 | — | — | 1 | 5.59 |
| CHEMBL5095897 | — | — | 1 | 5.57 |
| CHEMBL5093741 | — | — | 1 | 5.14 |
| CHEMBL4441878 | — | — | 1 | 5.02 |
| CHEMBL184574 | DEMETHYLBELLIDIFOLIN | — | 1 | - |
| CHEMBL5284529 | — | — | 1 | - |
| CHEMBL4783398 | — | — | 1 | - |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | - |
| CHEMBL140 | CURCUMIN | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4647659 | — | Kd | = | 0.046 | nM | 10.34 |
| CHEMBL1997924 | — | Kd | = | 1.952 | nM | 8.71 |
| CHEMBL5285332 | — | Kd | = | 3.745 | nM | 8.43 |
| CHEMBL393525 | — | Kd | = | 3.934 | nM | 8.40 |
| CHEMBL5289681 | — | Kd | = | 6.214 | nM | 8.21 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 7.673 | nM | 8.12 |
| CHEMBL4297639 | LORECIVIVINT | Kd | = | 155.07 | nM | 6.81 |
| CHEMBL3894571 | — | Kd | = | 159.94 | nM | 6.80 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 213.57 | nM | 6.67 |
| CHEMBL4873449 | — | Kd | = | 259.78 | nM | 6.58 |
| CHEMBL5279705 | — | Kd | = | 395.82 | nM | 6.40 |
| CHEMBL3589662 | — | Kd | = | 474.59 | nM | 6.32 |
| CHEMBL1802358 | — | Kd | = | 561.03 | nM | 6.25 |
| CHEMBL5081787 | — | Kd | = | 938.72 | nM | 6.03 |
| CHEMBL5086263 | — | Kd | = | 935.91 | nM | 6.03 |
| CHEMBL4784318 | CIRTUVIVINT | Kd | = | 1183.0 | nM | 5.93 |
| CHEMBL1614713 | CC-401 | Kd | = | 1277.58 | nM | 5.89 |
| CHEMBL1232500 | — | Kd | = | 1644.35 | nM | 5.78 |
| CHEMBL5091238 | — | Kd | = | 1762.17 | nM | 5.75 |
| CHEMBL3298236 | — | Kd | = | 1983.18 | nM | 5.70 |
| CHEMBL5283849 | — | Kd | = | 2515.78 | nM | 5.60 |
| CHEMBL4283240 | — | Kd | = | 2582.84 | nM | 5.59 |
| CHEMBL5095897 | — | Kd | = | 2705.19 | nM | 5.57 |
| CHEMBL5093741 | — | Kd | = | 7294.3 | nM | 5.14 |
| CHEMBL4441878 | — | Kd | = | 9586.0 | nM | 5.02 |
| CHEMBL3421968 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4292553 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL269538 | HARMINE | Kd | > | 10000.0 | nM | - |
| CHEMBL1236620 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5273528 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5070553 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4848254 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL140 | CURCUMIN | Kd | > | 10000.0 | nM | - |
| CHEMBL485053 | LEUCETTAMINE B | Kd | > | 10000.0 | nM | - |
| CHEMBL4783398 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL5284529 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL184574 | DEMETHYLBELLIDIFOLIN | Kd | > | 10000.0 | nM | - |