Assay Detail
Binding
CHEMBL5345759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TGFbetaR2 (unknown origin) autophosphorylation incubated for 45 to 60 mins in presence of ATP by [33P]-gammaATP based Topcount scintillation counting analysis
19
Total Activities
19
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
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 | 19 | 6.13 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5438171 | — | — | 1 | 7.84 |
| CHEMBL5401167 | — | — | 1 | 6.15 |
| CHEMBL5404502 | — | — | 1 | 6.11 |
| CHEMBL5395705 | — | — | 1 | 6.09 |
| CHEMBL5428147 | — | — | 1 | 6.06 |
| CHEMBL5412961 | — | — | 1 | 5.98 |
| CHEMBL5427025 | — | — | 1 | 5.90 |
| CHEMBL5431938 | — | — | 1 | 5.88 |
| CHEMBL5403558 | — | — | 1 | 5.88 |
| CHEMBL5415699 | — | — | 1 | 5.87 |
| CHEMBL5430774 | — | — | 1 | 5.70 |
| CHEMBL5396179 | — | — | 1 | - |
| CHEMBL5417490 | — | — | 1 | - |
| CHEMBL5397288 | — | — | 1 | - |
| CHEMBL5419476 | — | — | 1 | - |
| CHEMBL5420455 | — | — | 1 | - |
| CHEMBL5410107 | — | — | 1 | - |
| CHEMBL5400669 | — | — | 1 | - |
| CHEMBL5428443 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5438171 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL5401167 | — | IC50 | = | 703.2 | nM | 6.15 |
| CHEMBL5404502 | — | IC50 | = | 771.8 | nM | 6.11 |
| CHEMBL5395705 | — | IC50 | = | 818.1 | nM | 6.09 |
| CHEMBL5428147 | — | IC50 | = | 868.0 | nM | 6.06 |
| CHEMBL5412961 | — | IC50 | = | 1044.0 | nM | 5.98 |
| CHEMBL5427025 | — | IC50 | = | 1271.0 | nM | 5.90 |
| CHEMBL5431938 | — | IC50 | = | 1327.0 | nM | 5.88 |
| CHEMBL5403558 | — | IC50 | = | 1311.0 | nM | 5.88 |
| CHEMBL5415699 | — | IC50 | = | 1363.0 | nM | 5.87 |
| CHEMBL5430774 | — | IC50 | = | 1987.0 | nM | 5.70 |
| CHEMBL5396179 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5417490 | — | IC50 | - | — | - | |
| CHEMBL5397288 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5419476 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5420455 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5410107 | — | IC50 | - | — | - | |
| CHEMBL5400669 | — | IC50 | - | — | - | |
| CHEMBL5428443 | — | IC50 | - | — | - |