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Assay Detail

CHEMBL4026799

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

Binding
Inhibition of recombinant human ALK F1174L mutant (1093 to 1411 residues) expressed in baculovirus expression system using 5'FAM-KKSRGDYMTMQIG-CONH as substrate preincubated for 15 mins followed by addition of ATP measured after 1 hr by microfluidic mobility shift assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design.
Mah S, Park JH, Jung HY, Ahn K, Choi S, Tae HS, Jung KH, Rho JK, Lee JC, Hong SS, Hong S.
J Med Chem (2017) 60 : 9205 -9221
PubMed 29091425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.62 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.80
CHEMBL4065208 1 8.03
CHEMBL4091441 1 6.85
CHEMBL4087615 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 1.6 nM 8.80
CHEMBL4065208 IC50 = 9.3 nM 8.03
CHEMBL4091441 IC50 = 141.0 nM 6.85
CHEMBL4087615 IC50 = 154.0 nM 6.81