Assay Detail
Binding
CHEMBL5149645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His-Smt-tagged MSK1 C-terminal kinase domain (414 to 738 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using FAM-PSKPAATRKRRWSAPESR-NH2 as substrate preincubated for 1 hr followed by substrate addition and measured after 70 mins in presence of 250 uM by ADP-Glo kinase assay
5
Total Activities
5
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
Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.00 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5186781 | — | — | 1 | 6.70 |
| CHEMBL5187801 | — | — | 1 | 6.40 |
| CHEMBL5183977 | — | — | 1 | 6.10 |
| CHEMBL5208671 | — | — | 1 | 5.80 |
| CHEMBL5191771 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5186781 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL5187801 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5183977 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL5208671 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL5191771 | — | IC50 | = | 10000.0 | nM | 5.00 |