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Assay Detail

CHEMBL4003367

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

Binding
Inhibition of human CLK3 (275 to 632 residues) expressed in Escherichia coli BL21(DE3) preincubated for 10 mins followed by substrate addition by pyruvate kinase and lactate dehydrogenase coupled enzyme assay
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

Dual specificity protein kinase CLK3 (CHEMBL4226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.
Murár M, Dobiaš J, Šramel P, Addová G, Hanquet G, Boháč A.
Eur J Med Chem (2017) 126 : 754 -761
PubMed 27940419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.91 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261720 1 7.54
CHEMBL4090007 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261720 IC50 = 29.2 nM 7.54
CHEMBL4090007 IC50 = 530.0 nM 6.28