Assay Detail
Binding
CHEMBL5338277
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length SIK3 (unknown origin) using AMARA peptide as substrate incubated for 120 mins in presence of ATP by ADP-Glo kinase assay
26
Total Activities
26
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 |
Target
Serine/threonine-protein kinase SIK3 (CHEMBL6149) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.26 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5440720 | — | — | 1 | 9.22 |
| CHEMBL5417444 | — | — | 1 | 9.22 |
| CHEMBL5404502 | — | — | 1 | 8.85 |
| CHEMBL5402124 | — | — | 1 | 8.85 |
| CHEMBL5437300 | — | — | 1 | 8.77 |
| CHEMBL5439455 | — | — | 1 | 8.77 |
| CHEMBL5405883 | — | — | 1 | 8.77 |
| CHEMBL5410472 | — | — | 1 | 8.72 |
| CHEMBL5419090 | — | — | 1 | 8.51 |
| CHEMBL5440381 | — | — | 1 | 8.49 |
| CHEMBL5410039 | — | — | 1 | 8.44 |
| CHEMBL5393771 | — | — | 1 | 8.42 |
| CHEMBL5430610 | — | — | 1 | 8.38 |
| CHEMBL5420455 | — | — | 1 | 8.38 |
| CHEMBL5410109 | — | — | 1 | 8.36 |
| CHEMBL5426058 | — | — | 1 | 8.33 |
| CHEMBL5424512 | — | — | 1 | 8.22 |
| CHEMBL5421593 | — | — | 1 | 7.96 |
| CHEMBL5399976 | — | — | 1 | 7.94 |
| CHEMBL5412411 | — | — | 1 | 7.93 |
| CHEMBL5414213 | — | — | 1 | 7.85 |
| CHEMBL5399855 | — | — | 1 | 7.61 |
| CHEMBL5439601 | — | — | 1 | 7.46 |
| CHEMBL5417256 | — | — | 1 | 7.25 |
| CHEMBL5436639 | — | — | 1 | 7.24 |
| CHEMBL5410461 | — | — | 1 | 6.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5440720 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5417444 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5404502 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5402124 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5437300 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5439455 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5405883 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5410472 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5419090 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5440381 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5410039 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5393771 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5430610 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5420455 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5410109 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5426058 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5424512 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5421593 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL5399976 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL5412411 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL5414213 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL5399855 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL5439601 | — | IC50 | = | 34.4 | nM | 7.46 |
| CHEMBL5417256 | — | IC50 | = | 56.8 | nM | 7.25 |
| CHEMBL5436639 | — | IC50 | = | 58.2 | nM | 7.24 |
| CHEMBL5410461 | — | IC50 | = | 116.4 | nM | 6.93 |