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Assay Detail

CHEMBL5710019

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

Binding
Inhibition of His-tagged recombinant full length FES (unknown origin) expressed in baculovirus expression system
1
Total Activities
1
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

Tyrosine-protein kinase Fes/Fps (CHEMBL5455)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Zou HY, Li Q, Engstrom LD, West M, Appleman V, Wong KA, McTigue M, Deng YL, Liu W, Brooun A, Timofeevski S, McDonnell SR, Jiang P, Falk MD, Lappin PB, Affolter T, Nichols T, Hu W, Lam J, Johnson TW, Smeal T, Charest A, Fantin VR.
Proc Natl Acad Sci U S A (2015) 112 : 3493 -3498
PubMed 25733882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.22 8.22

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
CHEMBL5712062 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5712062 IC50 = 6.0 nM 8.22