Assay Detail
Binding
CHEMBL5327103
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length NanoLuc fused SIK1 (unknown origin) transfected in HEK293T cells using NanoBRET NanoGlo substrate incubated for 2 hrs in presence of tracer by NanoBRET assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase SIK1 (CHEMBL6082) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Shifting the selectivity of pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.93 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5402213 | — | — | 1 | 8.22 |
| CHEMBL5090394 | — | — | 1 | 7.92 |
| CHEMBL5401391 | — | — | 1 | 7.70 |
| CHEMBL3770443 | — | — | 1 | 7.48 |
| CHEMBL5425418 | — | — | 1 | 7.14 |
| CHEMBL5423817 | — | — | 1 | 6.64 |
| CHEMBL5415867 | — | — | 1 | 6.62 |
| CHEMBL5416418 | — | — | 1 | 6.56 |
| CHEMBL5409353 | — | — | 1 | 6.37 |
| CHEMBL5417915 | — | — | 1 | 6.00 |
| CHEMBL5438800 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5402213 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5090394 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5401391 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3770443 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5425418 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5423817 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL5415867 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL5416418 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL5409353 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL5417915 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5438800 | — | IC50 | = | 2400.0 | nM | 5.62 |