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Assay Detail

CHEMBL4031765

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

Binding
Inhibition of CLK2 in human HCT116 cell lysate after 1 hr by LC-MS/MS analysis relative to control
1
Total Activities
1
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

The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic Screen.
Riggs JR, Nagy M, Elsner J, Erdman P, Cashion D, Robinson D, Harris R, Huang D, Tehrani L, Deyanat-Yazdi G, Narla RK, Peng X, Tran T, Barnes L, Miller T, Katz J, Tang Y, Chen M, Moghaddam MF, Bahmanyar S, Pagarigan B, Delker S, LeBrun L, Chamberlain PP, Calabrese A, Canan SS, Leftheris K, Zhu D, Boylan JF.
J Med Chem (2017) 60 : 8989 -9002
PubMed 28991472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.82 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062218 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062218 IC50 = 15.0 nM 7.82