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Assay Detail

CHEMBL5720225

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

Binding
Inhibition of recombinant human full-length N-terminal GST-tagged CK1epsilon expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 60 mins by ADP-glo kinase assay
4
Total Activities
4
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

Casein kinase I isoform epsilon (CHEMBL4937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Deng C, Lipstein MR, Scotto L, Jirau Serrano XO, Mangone MA, Li S, Vendome J, Hao Y, Xu X, Deng SX, Realubit RB, Tatonetti NP, Karan C, Lentzsch S, Fruman DA, Honig B, Landry DW, O'Connor OA.
Blood (2017) 129 : 88 -99
PubMed 27784673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.62 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2069623 1 8.13
CHEMBL3948730 UMBRALISIB 4.0 1 5.22
CHEMBL5722968 1 5.03
CHEMBL5722975 1 4.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2069623 EC50 = 7.4 nM 8.13
CHEMBL3948730 UMBRALISIB EC50 = 6000.0 nM 5.22
CHEMBL5722968 EC50 = 9362.0 nM 5.03
CHEMBL5722975 EC50 = 81180.0 nM 4.09