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Assay Detail

CHEMBL5098261

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

Binding
Binding affinity to ALK (unknown origin) using TK as substrate incubated for 1 hr in presence of ATP by HTRF analysis
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

ALK tyrosine kinase receptor (CHEMBL4247)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK).
Xie S, Sun Y, Liu Y, Li X, Li X, Zhong W, Zhan F, Zhu J, Yao H, Yang DH, Chen ZS, Xu J, Xu S.
J Med Chem (2021) 64 : 9120 -9140
PubMed 34176264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.68 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4859551 1 6.54
CHEMBL3747525 1 6.50
CHEMBL1738797 ALECTINIB 4.0 1 5.99
CHEMBL4875115 1 4.87
CHEMBL5188519 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4859551 IC50 = 290.0 nM 6.54
CHEMBL3747525 IC50 = 320.0 nM 6.50
CHEMBL1738797 ALECTINIB IC50 = 1030.0 nM 5.99
CHEMBL4875115 IC50 = 13630.0 nM 4.87
CHEMBL5188519 IC50 = 30630.0 nM 4.51