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Assay Detail

CHEMBL5665067

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

Binding
Inhibition of human N-terminal GST-fused ROS cytoplasmic domain (1883 to 2347(end) residues) expressed in baculovirus expression system using IRS1 as substrate measured after 1 hr by off-chip mobility shift assay relative to control
2
Total Activities
2
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

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

Target

Proto-oncogene tyrosine-protein kinase ROS (CHEMBL5568)
Type SINGLE 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
IC50 2 8.54 9.02

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
CHEMBL601719 CRIZOTINIB 4.0 1 9.02
CHEMBL3545360 ASP-3026 1.0 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL601719 CRIZOTINIB IC50 = 0.95 nM 9.02
CHEMBL3545360 ASP-3026 IC50 = 8.9 nM 8.05