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

CHEMBL3607766

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

Binding
Inhibition of RSK2 in mouse BAF cells expressing activated FGFR assessed as reduction of YB1 phosphorylation at Ser102 by electochemiluminescence assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BAF
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ribosomal protein S6 kinase alpha-3 (CHEMBL3297641)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Potent and Selective RSK Inhibitors as Biological Probes.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Lindvall M, Appleton BA, Shafer CM.
J Med Chem (2015) 58 : 6766 -6783
PubMed 26270416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 35 5.86 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3604792 1 6.85
CHEMBL3604794 1 6.68
CHEMBL3604793 1 6.47
CHEMBL3604885 1 6.44
CHEMBL3604881 1 6.36
CHEMBL3604784 1 6.31
CHEMBL3604889 1 6.30
CHEMBL3604882 1 6.24
CHEMBL3604888 1 6.21
CHEMBL3604884 1 6.16
CHEMBL3604886 1 6.16
CHEMBL3604785 1 5.96
CHEMBL3604787 1 5.96
CHEMBL3604790 1 5.96
CHEMBL3604775 1 5.85
CHEMBL3604887 1 5.82
CHEMBL3604789 1 5.80
CHEMBL3604791 1 5.68
CHEMBL3604779 1 5.66
CHEMBL3604786 1 5.64
CHEMBL3604883 1 5.60
CHEMBL3604771 1 5.55
CHEMBL3604774 1 5.50
CHEMBL3604782 1 5.39
CHEMBL3604778 1 5.38
CHEMBL3604795 1 5.28
CHEMBL3604783 1 5.25
CHEMBL3604777 1 5.19
CHEMBL3604776 1 5.03
CHEMBL3604788 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3604792 EC50 = 140.0 nM 6.85
CHEMBL3604794 EC50 = 210.0 nM 6.68
CHEMBL3604793 EC50 = 340.0 nM 6.47
CHEMBL3604885 EC50 = 360.0 nM 6.44
CHEMBL3604881 EC50 = 440.0 nM 6.36
CHEMBL3604784 EC50 = 490.0 nM 6.31
CHEMBL3604889 EC50 = 500.0 nM 6.30
CHEMBL3604882 EC50 = 580.0 nM 6.24
CHEMBL3604888 EC50 = 610.0 nM 6.21
CHEMBL3604884 EC50 = 690.0 nM 6.16
CHEMBL3604886 EC50 = 690.0 nM 6.16
CHEMBL3604785 EC50 = 1100.0 nM 5.96
CHEMBL3604787 EC50 = 1100.0 nM 5.96
CHEMBL3604790 EC50 = 1100.0 nM 5.96
CHEMBL3604775 EC50 = 1400.0 nM 5.85
CHEMBL3604887 EC50 = 1500.0 nM 5.82
CHEMBL3604789 EC50 = 1600.0 nM 5.80
CHEMBL3604791 EC50 = 2100.0 nM 5.68
CHEMBL3604779 EC50 = 2200.0 nM 5.66
CHEMBL3604786 EC50 = 2300.0 nM 5.64
CHEMBL3604883 EC50 = 2500.0 nM 5.60
CHEMBL3604771 EC50 = 2800.0 nM 5.55
CHEMBL3604774 EC50 = 3200.0 nM 5.50
CHEMBL3604782 EC50 = 4100.0 nM 5.39
CHEMBL3604778 EC50 = 4200.0 nM 5.38
CHEMBL3604795 EC50 = 5300.0 nM 5.28
CHEMBL3604783 EC50 = 5600.0 nM 5.25
CHEMBL3604777 EC50 = 6400.0 nM 5.19
CHEMBL3604776 EC50 = 9300.0 nM 5.03
CHEMBL3604788 EC50 = 10400.0 nM 4.98
CHEMBL3604796 EC50 > 20000.0 nM -
CHEMBL3604772 EC50 > 20000.0 nM -
CHEMBL3604773 EC50 > 20000.0 nM -
CHEMBL3604780 EC50 > 20000.0 nM -
CHEMBL3604781 EC50 > 20000.0 nM -