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Assay Detail

CHEMBL3386213

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

Binding
Inhibition of GST-tagged rat CK1delta expressed in Escherichia coli using GST-p53 (1 to 64 residues) by SDS-PAGE based autoradiography
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Casein kinase I isoform delta (CHEMBL4484)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 10 6.74 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3337845 1 7.70
CHEMBL3337854 1 7.40
CHEMBL3337850 1 6.89
CHEMBL3337846 1 6.85
CHEMBL3337849 1 6.68
CHEMBL3337851 1 6.58
CHEMBL3337852 1 6.52
CHEMBL3337853 1 6.26
CHEMBL3337847 1 6.25
CHEMBL3337848 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3337845 IC50 = 20.0 nM 7.70
CHEMBL3337854 IC50 = 40.0 nM 7.40
CHEMBL3337850 IC50 = 130.0 nM 6.89
CHEMBL3337846 IC50 = 140.0 nM 6.85
CHEMBL3337849 IC50 = 210.0 nM 6.68
CHEMBL3337851 IC50 = 260.0 nM 6.58
CHEMBL3337852 IC50 = 300.0 nM 6.52
CHEMBL3337853 IC50 = 550.0 nM 6.26
CHEMBL3337847 IC50 = 560.0 nM 6.25
CHEMBL3337848 IC50 = 570.0 nM 6.24