Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5149648

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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 measured after 70 mins by ADP-Glo kinase assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ribosomal protein S6 kinase alpha-5 (CHEMBL4237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.
Hall A, Abendroth J, Bolejack MJ, Ceska T, Dell'Aiera S, Ellis V, Fox D, François C, Muruthi MM, Prével C, Poullennec K, Romanov S, Valade A, Vanbellinghen A, Yano J, Geraerts M.
ACS Med Chem Lett (2022) 13 : 1099 -1108
PubMed 35859861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.80 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187801 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187801 IC50 = 15848.93 nM 4.80