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Assay Detail

CHEMBL2350997

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

Binding
Inhibition of RSK2 (unknown origin) using AKRRRLSSLRA as substrate after 60 mins by fluorescence assay
41
Total Activities
41
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

Target

Ribosomal protein S6 kinase alpha-3 (CHEMBL2345)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.
Zhong Y, Xue M, Zhao X, Yuan J, Liu X, Huang J, Zhao Z, Li H, Xu Y.
Bioorg Med Chem (2013) 21 : 1724 -1734
PubMed 23434140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 5.56 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347053 1 6.30
CHEMBL2347075 1 5.82
CHEMBL2347061 1 5.78
CHEMBL2347074 1 5.70
CHEMBL2347085 1 5.60
CHEMBL1778710 1 5.57
CHEMBL2347073 1 5.46
CHEMBL2347054 1 5.07
CHEMBL2347062 1 4.77
CHEMBL2346669 1 -
CHEMBL2347052 1 -
CHEMBL2347055 1 -
CHEMBL2347066 1 -
CHEMBL1595681 1 -
CHEMBL2347071 1 -
CHEMBL2347070 1 -
CHEMBL2347069 1 -
CHEMBL572335 1 -
CHEMBL2347068 1 -
CHEMBL2347051 1 -
CHEMBL2347086 1 -
CHEMBL2347076 1 -
CHEMBL2347084 1 -
CHEMBL2347077 1 -
CHEMBL2347083 1 -
CHEMBL2347082 1 -
CHEMBL2347081 1 -
CHEMBL2347080 1 -
CHEMBL2347079 1 -
CHEMBL2347078 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347053 IC50 = 500.0 nM 6.30
CHEMBL2347075 IC50 = 1510.0 nM 5.82
CHEMBL2347061 IC50 = 1680.0 nM 5.78
CHEMBL2347074 IC50 = 2020.0 nM 5.70
CHEMBL2347085 IC50 = 2490.0 nM 5.60
CHEMBL1778710 IC50 = 2720.0 nM 5.57
CHEMBL2347073 IC50 = 3470.0 nM 5.46
CHEMBL2347054 IC50 = 8590.0 nM 5.07
CHEMBL2347062 IC50 = 17000.0 nM 4.77
CHEMBL2347071 IC50 - -
CHEMBL2347056 IC50 - -
CHEMBL2347070 IC50 - -
CHEMBL2347069 IC50 - -
CHEMBL572335 IC50 - -
CHEMBL2347068 IC50 - -
CHEMBL2347067 IC50 - -
CHEMBL371713 IC50 - -
CHEMBL2347072 IC50 - -
CHEMBL2347065 IC50 - -
CHEMBL2347064 IC50 - -
CHEMBL2347063 IC50 - -
CHEMBL2347060 IC50 - -
CHEMBL2347059 IC50 - -
CHEMBL2347058 IC50 - -
CHEMBL2347057 IC50 - -
CHEMBL1595681 IC50 - -
CHEMBL2347066 IC50 - -
CHEMBL2347055 IC50 - -
CHEMBL2347052 IC50 - -
CHEMBL2346669 IC50 - -
CHEMBL2347051 IC50 - -
CHEMBL2347086 IC50 - -
CHEMBL2347076 IC50 - -
CHEMBL2347084 IC50 - -
CHEMBL2347077 IC50 - -
CHEMBL2347083 IC50 - -
CHEMBL2347082 IC50 - -
CHEMBL2347081 IC50 - -
CHEMBL2347080 IC50 - -
CHEMBL2347079 IC50 - -
CHEMBL2347078 IC50 - -