Assay Detail
Toxicity
CHEMBL5338275
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Inhibition of N-terminal GST-tagged wild type human SIK1 (1 to 783 residues) expressed in baculovirus-infected Sf21 cells 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 | Toxicity |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase SIK1 (CHEMBL6082) ↗| 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 | 7.12 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5417444 | — | — | 1 | 8.70 |
| CHEMBL5440720 | — | — | 1 | 8.21 |
| CHEMBL5399976 | — | — | 1 | 8.00 |
| CHEMBL5404502 | — | — | 1 | 7.97 |
| CHEMBL5405883 | — | — | 1 | 7.78 |
| CHEMBL5420455 | — | — | 1 | 7.67 |
| CHEMBL5439455 | — | — | 1 | 7.57 |
| CHEMBL5399855 | — | — | 1 | 7.41 |
| CHEMBL5402124 | — | — | 1 | 7.35 |
| CHEMBL5437300 | — | — | 1 | 7.29 |
| CHEMBL5410472 | — | — | 1 | 7.21 |
| CHEMBL5424512 | — | — | 1 | 7.20 |
| CHEMBL5430610 | — | — | 1 | 7.10 |
| CHEMBL5419090 | — | — | 1 | 7.08 |
| CHEMBL5410109 | — | — | 1 | 6.95 |
| CHEMBL5440381 | — | — | 1 | 6.77 |
| CHEMBL5414213 | — | — | 1 | 6.74 |
| CHEMBL5410039 | — | — | 1 | 6.62 |
| CHEMBL5393771 | — | — | 1 | 6.55 |
| CHEMBL5426058 | — | — | 1 | 6.50 |
| CHEMBL5439601 | — | — | 1 | 6.31 |
| CHEMBL5421593 | — | — | 1 | 6.16 |
| CHEMBL5417256 | — | — | 1 | 6.06 |
| CHEMBL5412411 | — | — | 1 | 5.79 |
| CHEMBL5436639 | — | — | 1 | - |
| CHEMBL5410461 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5417444 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5440720 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5399976 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5404502 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5405883 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL5420455 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL5439455 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5399855 | — | IC50 | = | 38.6 | nM | 7.41 |
| CHEMBL5402124 | — | IC50 | = | 44.9 | nM | 7.35 |
| CHEMBL5437300 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL5410472 | — | IC50 | = | 61.1 | nM | 7.21 |
| CHEMBL5424512 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5430610 | — | IC50 | = | 79.7 | nM | 7.10 |
| CHEMBL5419090 | — | IC50 | = | 82.5 | nM | 7.08 |
| CHEMBL5410109 | — | IC50 | = | 112.9 | nM | 6.95 |
| CHEMBL5440381 | — | IC50 | = | 169.2 | nM | 6.77 |
| CHEMBL5414213 | — | IC50 | = | 183.7 | nM | 6.74 |
| CHEMBL5410039 | — | IC50 | = | 240.2 | nM | 6.62 |
| CHEMBL5393771 | — | IC50 | = | 282.8 | nM | 6.55 |
| CHEMBL5426058 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL5439601 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5421593 | — | IC50 | = | 699.8 | nM | 6.16 |
| CHEMBL5417256 | — | IC50 | = | 866.7 | nM | 6.06 |
| CHEMBL5412411 | — | IC50 | = | 1639.0 | nM | 5.79 |
| CHEMBL5436639 | — | IC50 | > | 2633.0 | nM | - |
| CHEMBL5410461 | — | IC50 | > | 3763.0 | nM | - |