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Assay Detail

CHEMBL5501743

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

Binding
Inhibition of recombinant human TLK2 (388 to end residues) using myelin basic protein as substrate incubated for 2 hrs in presence of ATP by ADP-Glo kinase assay
5
Total Activities
5
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

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

Publication

Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.
Asquith CRM, East MP, Laitinen T, Alamillo-Ferrer C, Hartikainen E, Wells CI, Axtman AD, Drewry DH, Tizzard GJ, Poso A, Willson TM, Johnson GL.
Eur J Med Chem (2024) 271 : 116357 -116357
PubMed 38636130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.32 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5555013 1 7.01
CHEMBL5555697 1 6.60
CHEMBL258805 SU-9516 1.0 1 6.55
CHEMBL5542619 1 6.35
CHEMBL5542714 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5555013 IC50 = 97.0 nM 7.01
CHEMBL5555697 IC50 = 250.0 nM 6.60
CHEMBL258805 SU-9516 IC50 = 280.0 nM 6.55
CHEMBL5542619 IC50 = 450.0 nM 6.35
CHEMBL5542714 IC50 = 7800.0 nM 5.11