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Assay Detail

CHEMBL4705509

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

Binding
Inhibition of human ALK S1206Y mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.
Chen J,Zhou Y,Dong X,Liu L,Bai L,McEachern D,Przybranowski S,Yang CY,Stuckey J,Li X,Wen B,Zhao T,Sun S,Sun D,Jiao L,Jing Y,Guo M,Yang D,Wang S
J Med Chem (2020) 63 : 13994 -14016
PubMed 33185101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.96 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1738797 ALECTINIB 4.0 1 9.02
CHEMBL2403108 CERITINIB 4.0 1 8.80
CHEMBL4764610 1 8.05
CHEMBL601719 CRIZOTINIB 4.0 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1738797 ALECTINIB IC50 = 0.96 nM 9.02
CHEMBL2403108 CERITINIB IC50 = 1.6 nM 8.80
CHEMBL4764610 IC50 = 8.9 nM 8.05
CHEMBL601719 CRIZOTINIB IC50 = 1066.0 nM 5.97