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Assay Detail

CHEMBL2020792

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

Binding
Inhibition of His-tagged RSK2 expressed in Sf9 cells using ERalpha-Ser167 RLASTND as substrate after 120 mins by chemiluminescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
Hilinski MK, Mrozowski RM, Clark DE, Lannigan DA.
Bioorg Med Chem Lett (2012) 22 : 3244 -3247
PubMed 22464132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.15 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2017518 1 6.60
CHEMBL2017522 1 6.45
CHEMBL2017521 1 6.31
CHEMBL240954 1 6.23
CHEMBL2017519 1 6.06
CHEMBL2017517 1 5.95
CHEMBL2017523 1 5.84
CHEMBL2017520 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2017518 IC50 = 252.0 nM 6.60
CHEMBL2017522 IC50 = 356.0 nM 6.45
CHEMBL2017521 IC50 = 493.0 nM 6.31
CHEMBL240954 IC50 = 583.0 nM 6.23
CHEMBL2017519 IC50 = 869.0 nM 6.06
CHEMBL2017517 IC50 = 1130.0 nM 5.95
CHEMBL2017523 IC50 = 1430.0 nM 5.84
CHEMBL2017520 IC50 = 1920.0 nM 5.72