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Assay Detail

CHEMBL4016846

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

Binding
Inhibition of recombinant human GST-tagged Clk1 expressed in Escherichia coli using RS repeat substrate peptide after 15 mins in presence of [gamma-32]-ATP
21
Total Activities
21
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

Dual specificity protein kinase CLK1 (CHEMBL4224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Selective Clk1 and -4 Inhibitors for Cellular Depletion of Cancer-Relevant Proteins.
ElHady AK, Abdel-Halim M, Abadi AH, Engel M.
J Med Chem (2017) 60 : 5377 -5391
PubMed 28561591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.33 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4082113 1 8.16
CHEMBL4085557 1 7.35
CHEMBL4070477 1 7.09
CHEMBL4103654 1 7.08
CHEMBL4064016 1 6.97
CHEMBL4077249 1 -
CHEMBL4076404 1 -
CHEMBL4064365 1 -
CHEMBL4088454 1 -
CHEMBL4064031 1 -
CHEMBL4075340 1 -
CHEMBL4093645 1 -
CHEMBL4102695 1 -
CHEMBL4077343 1 -
CHEMBL4094065 1 -
CHEMBL4099320 1 -
CHEMBL4072371 1 -
CHEMBL4067725 1 -
CHEMBL4094143 1 -
CHEMBL4065656 1 -
CHEMBL4075996 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4082113 IC50 = 6.9 nM 8.16
CHEMBL4085557 IC50 = 45.0 nM 7.35
CHEMBL4070477 IC50 = 81.6 nM 7.09
CHEMBL4103654 IC50 = 84.0 nM 7.08
CHEMBL4064016 IC50 = 107.0 nM 6.97
CHEMBL4077249 IC50 - -
CHEMBL4076404 IC50 - -
CHEMBL4064365 IC50 - -
CHEMBL4088454 IC50 - -
CHEMBL4064031 IC50 - -
CHEMBL4075340 IC50 - -
CHEMBL4093645 IC50 - -
CHEMBL4102695 IC50 - -
CHEMBL4077343 IC50 - -
CHEMBL4094065 IC50 - -
CHEMBL4099320 IC50 - -
CHEMBL4072371 IC50 - -
CHEMBL4067725 IC50 - -
CHEMBL4094143 IC50 - -
CHEMBL4065656 IC50 - -
CHEMBL4075996 IC50 - -