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Assay Detail

CHEMBL2328037

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

Binding
Inhibition of recombinant RSK2 (unknown origin) expressed in baculovirus infected Sf9 cells assessed as decrease in substrate phosphorylation using GST-fusion protein containing ERalpha-Ser167 sequence-RLASTND as substrate by chemiluminescence analysis
8
Total Activities
8
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-3 (CHEMBL2345)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Improving the affinity of SL0101 for RSK using structure-based design.
Mrozowski RM, Vemula R, Wu B, Zhang Q, Schroeder BR, Hilinski MK, Clark DE, Hecht SM, O'Doherty GA, Lannigan DA.
ACS Med Chem Lett (2013) 4 : 175 -179
PubMed 23519677 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.22 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2321925 1 7.70
CHEMBL2326706 1 6.32
CHEMBL2326708 1 6.21
CHEMBL2326705 1 6.15
CHEMBL240954 1 6.00
CHEMBL2326707 1 5.82
CHEMBL2326704 1 5.82
CHEMBL2326709 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2321925 IC50 = 20.0 nM 7.70
CHEMBL2326706 IC50 = 480.0 nM 6.32
CHEMBL2326708 IC50 = 620.0 nM 6.21
CHEMBL2326705 IC50 = 710.0 nM 6.15
CHEMBL240954 IC50 = 990.0 nM 6.00
CHEMBL2326707 IC50 = 1500.0 nM 5.82
CHEMBL2326704 IC50 = 1510.0 nM 5.82
CHEMBL2326709 IC50 = 1770.0 nM 5.75