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Assay Detail

CHEMBL5149640

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

Binding
Inhibition of MSK2 (unknown origin) FAM-PSKPAATRKRRWSAPESR-NH2 as substrate preincubated for 1 hr followed by activation with ERK2 and substrate addition measured after 2 hrs by microfluidic chip based electrophoresis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ribosomal protein S6 kinase alpha-4 (CHEMBL3125)
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 5 6.38 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5184056 1 7.70
CHEMBL5190298 1 7.10
CHEMBL5187801 1 6.10
CHEMBL5183977 1 5.50
CHEMBL5198790 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5184056 IC50 = 19.95 nM 7.70
CHEMBL5190298 IC50 = 79.43 nM 7.10
CHEMBL5187801 IC50 = 794.33 nM 6.10
CHEMBL5183977 IC50 = 3162.28 nM 5.50
CHEMBL5198790 IC50 = 3162.28 nM 5.50