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Assay Detail

CHEMBL3831013

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

Binding
Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H3122
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.
Song Z, Xia Z, Ji Y, Xing L, Gao Y, Ai J, Geng M, Zhang A.
Eur J Med Chem (2016) 118 : 244 -249
PubMed 27131066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.25 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3735648 1 7.75
CHEMBL1738797 ALECTINIB 4.0 1 7.72
CHEMBL3735386 1 7.31
CHEMBL3736388 1 6.90
CHEMBL601719 CRIZOTINIB 4.0 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3735648 IC50 = 17.9 nM 7.75
CHEMBL1738797 ALECTINIB IC50 = 19.0 nM 7.72
CHEMBL3735386 IC50 = 49.0 nM 7.31
CHEMBL3736388 IC50 = 126.0 nM 6.90
CHEMBL601719 CRIZOTINIB IC50 = 261.0 nM 6.58