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Assay Detail

CHEMBL3386219

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

Binding
Inhibition of human recombinant CK1epsilon expressed in Escherichia coli using alpha casein substrate by SDS-PAGE based autoradiography
2
Total Activities
2
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

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

Publication

Difluoro-dioxolo-benzoimidazol-benzamides as potent inhibitors of CK1δ and ε with nanomolar inhibitory activity on cancer cell proliferation.
Richter J, Bischof J, Zaja M, Kohlhof H, Othersen O, Vitt D, Alscher V, Pospiech I, García-Reyes B, Berg S, Leban J, Knippschild U.
J Med Chem (2014) 57 : 7933 -7946
PubMed 25191940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.76 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3337846 1 6.80
CHEMBL3337845 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3337846 IC50 = 160.0 nM 6.80
CHEMBL3337845 IC50 = 190.0 nM 6.72