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Assay Detail

CHEMBL4189210

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Binding
Inhibition of human recombinant CK1epsilon using alpha-casein as substrate after 30 mins in presence of [gamma-32P]-ATP by Cherenkov counting method
11
Total Activities
11
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

Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε.
García-Reyes B, Witt L, Jansen B, Karasu E, Gehring T, Leban J, Henne-Bruns D, Pichlo C, Brunstein E, Baumann U, Wesseler F, Rathmer B, Schade D, Peifer C, Knippschild U.
J Med Chem (2018) 61 : 4087 -4102
PubMed 29630366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.58 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204681 1 6.25
CHEMBL4213046 1 5.91
CHEMBL4212803 1 5.85
CHEMBL1257064 1 5.39
CHEMBL2324266 1 5.38
CHEMBL1257090 1 5.15
CHEMBL1257114 1 5.13
CHEMBL1257089 1 -
CHEMBL4208290 1 -
CHEMBL4215433 1 -
CHEMBL4209726 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204681 IC50 = 560.0 nM 6.25
CHEMBL4213046 IC50 = 1230.0 nM 5.91
CHEMBL4212803 IC50 = 1410.0 nM 5.85
CHEMBL1257064 IC50 = 4030.0 nM 5.39
CHEMBL2324266 IC50 = 4120.0 nM 5.38
CHEMBL1257090 IC50 = 7070.0 nM 5.15
CHEMBL1257114 IC50 = 7340.0 nM 5.13
CHEMBL1257089 IC50 > 10000.0 nM -
CHEMBL4208290 IC50 - -
CHEMBL4215433 IC50 - -
CHEMBL4209726 IC50 - -