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Assay Detail

CHEMBL4841342

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

Binding
Inhibition of RSK4 (unknown origin) incubated for 40 mins in presence of ATP and lipid substrate by Kinase-Glo plus luminescence assay
24
Total Activities
24
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-6 (CHEMBL4924)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Optimization, and Structure-Activity Relationship Study of Novel and Potent RSK4 Inhibitors as Promising Agents for the Treatment of Esophageal Squamous Cell Carcinoma.
Yuan Y, Xu J, Jiang L, Yu K, Ge Y, Li M, He H, Niu Q, Shi X, Fan L, Chen Z, Zhao Z, Li S, Xu Y, Wang Z, Li H.
J Med Chem (2021) 64 : 13572 -13587
PubMed 34496560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.65 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4847762 1 8.02
CHEMBL573107 1 7.94
CHEMBL4846725 1 7.92
CHEMBL4847469 1 7.92
CHEMBL4870231 1 7.82
CHEMBL4870807 1 7.81
CHEMBL4846978 1 7.75
CHEMBL4845942 1 7.60
CHEMBL4872665 1 7.54
CHEMBL4852908 1 7.48
CHEMBL4850890 1 7.26
CHEMBL4856762 1 7.08
CHEMBL4869608 1 6.93
CHEMBL4852557 1 6.52
CHEMBL4850184 1 6.40
CHEMBL4874868 1 6.39
CHEMBL4865220 1 5.67
CHEMBL4846647 1 5.45
CHEMBL4866663 1 5.33
CHEMBL4868071 1 5.13
CHEMBL4871187 1 5.01
CHEMBL4848180 1 4.98
CHEMBL4854622 1 4.86
CHEMBL4849875 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4847762 IC50 = 9.5 nM 8.02
CHEMBL573107 IC50 = 11.5 nM 7.94
CHEMBL4846725 IC50 = 12.0 nM 7.92
CHEMBL4847469 IC50 = 12.0 nM 7.92
CHEMBL4870231 IC50 = 15.0 nM 7.82
CHEMBL4870807 IC50 = 15.5 nM 7.81
CHEMBL4846978 IC50 = 18.0 nM 7.75
CHEMBL4845942 IC50 = 25.0 nM 7.60
CHEMBL4872665 IC50 = 28.5 nM 7.54
CHEMBL4852908 IC50 = 33.0 nM 7.48
CHEMBL4850890 IC50 = 54.9 nM 7.26
CHEMBL4856762 IC50 = 84.0 nM 7.08
CHEMBL4869608 IC50 = 117.0 nM 6.93
CHEMBL4852557 IC50 = 300.5 nM 6.52
CHEMBL4850184 IC50 = 395.0 nM 6.40
CHEMBL4874868 IC50 = 410.0 nM 6.39
CHEMBL4865220 IC50 = 2118.0 nM 5.67
CHEMBL4846647 IC50 = 3588.0 nM 5.45
CHEMBL4866663 IC50 = 4725.0 nM 5.33
CHEMBL4868071 IC50 = 7343.5 nM 5.13
CHEMBL4871187 IC50 = 9735.0 nM 5.01
CHEMBL4848180 IC50 = 10567.0 nM 4.98
CHEMBL4854622 IC50 = 13781.0 nM 4.86
CHEMBL4849875 IC50 = 17627.0 nM 4.75