Assay Detail
Binding
CHEMBL5345753
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SIK3 isoform 1 (59 to 1321 residues) expressed in Sf9 insect cells using AMARA peptide as substrate incubated for 120 mins in presence of ATP by ADP-Glo assay
21
Total Activities
21
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 |
Target
Serine/threonine-protein kinase SIK3 (CHEMBL6149) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.30 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5417444 | — | — | 1 | 9.22 |
| CHEMBL5438171 | — | — | 1 | 9.00 |
| CHEMBL5431938 | — | — | 1 | 9.00 |
| CHEMBL5415380 | — | — | 1 | 8.96 |
| CHEMBL5412961 | — | — | 1 | 8.89 |
| CHEMBL5404502 | — | — | 1 | 8.85 |
| CHEMBL5397288 | — | — | 1 | 8.66 |
| CHEMBL5401167 | — | — | 1 | 8.54 |
| CHEMBL5427025 | — | — | 1 | 8.43 |
| CHEMBL5420455 | — | — | 1 | 8.38 |
| CHEMBL5396179 | — | — | 1 | 8.38 |
| CHEMBL5403558 | — | — | 1 | 8.36 |
| CHEMBL5415699 | — | — | 1 | 8.30 |
| CHEMBL5419476 | — | — | 1 | 8.18 |
| CHEMBL5395705 | — | — | 1 | 8.17 |
| CHEMBL5430774 | — | — | 1 | 7.99 |
| CHEMBL5428147 | — | — | 1 | 7.91 |
| CHEMBL5428443 | — | — | 1 | 7.28 |
| CHEMBL5410107 | — | — | 1 | 6.79 |
| CHEMBL5417490 | — | — | 1 | 6.73 |
| CHEMBL5400669 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5417444 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5438171 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5431938 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5415380 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5412961 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5404502 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5397288 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5401167 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5427025 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5420455 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5396179 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5403558 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5415699 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5419476 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5395705 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5430774 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5428147 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL5428443 | — | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL5410107 | — | IC50 | = | 163.7 | nM | 6.79 |
| CHEMBL5417490 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL5400669 | — | IC50 | > | 4000.0 | nM | - |