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Assay Detail

CHEMBL5665134

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

Binding
Inhibition of EML4-ALK (unknown origin) expressed in mouse 3T3 cells assessed as growth inhibition measured after 2 days by celltiter-glo luminescent cell viability assay
4
Total Activities
2
Compounds Tested
2
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 3T3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

EML4-ALK (CHEMBL3883330)
Type CHIMERIC PROTEIN
Organism Homo sapiens

Publication

The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice.
Mori M, Ueno Y, Konagai S, Fushiki H, Shimada I, Kondoh Y, Saito R, Mori K, Shindou N, Soga T, Sakagami H, Furutani T, Doihara H, Kudoh M, Kuromitsu S.
Mol Cancer Ther (2014) 13 : 329 -340
PubMed 24419060 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
GI 2 - -
IC50 2 7.37 7.38

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0003060
EFO_TERM EFO_TERM - non-small cell lung carcinoma

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545360 ASP-3026 1.0 2 7.38
CHEMBL601719 CRIZOTINIB 4.0 2 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545360 ASP-3026 IC50 = 42.0 nM 7.38
CHEMBL601719 CRIZOTINIB IC50 = 45.0 nM 7.35
CHEMBL3545360 ASP-3026 GI - -
CHEMBL601719 CRIZOTINIB GI - -