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Assay Detail

CHEMBL4266500

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

Binding
Inhibition of recombinant human GST-tagged CLK2 catalytic domain (137 to 498 residues) expressed in baculovirus expression system in presence of 25 uM ATP
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 CLK2 (CHEMBL4225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Degorce SL, Anjum R, Dillman KS, Drew L, Groombridge SD, Halsall CT, Lenz EM, Lindsay NA, Mayo MF, Pink JH, Robb GR, Scott JS, Stokes S, Xue Y.
Bioorg Med Chem (2018) 26 : 913 -924
PubMed 29398441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.09 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4290222 1 7.41
CHEMBL4278882 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4290222 IC50 = 39.0 nM 7.41
CHEMBL4278882 IC50 = 175.0 nM 6.76