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Assay Detail

CHEMBL5144097

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

Binding
Binding affinity to full length FLAG/HA/Strep-tagged TLK2 (388 to 772 residues) (unknown origin) transfected in HEK293T cells by Alexa Fluor 647 staining based FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase tousled-like 2 (CHEMBL5404)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of bisindole derivatives as anticancer agents against Tousled-like kinases.
Lee SB, Chang TY, Lee NZ, Yu ZY, Liu CY, Lee HY.
Eur J Med Chem (2022) 227 : 113904 -113904
PubMed 34662748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.33 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5204542 1 7.73
CHEMBL5188455 1 7.48
CHEMBL5173181 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5204542 IC50 = 18.65 nM 7.73
CHEMBL5188455 IC50 = 33.15 nM 7.48
CHEMBL5173181 IC50 = 163.4 nM 6.79