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Assay Detail

CHEMBL1926253

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

Binding
Inhibition of human GST-tagged ALK expressed in SF21 insect cells using PLCgamma/GST as substrate after 15 mins by time-resolved fluorescence assay
2
Total Activities
2
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

2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Weinberg LR, Albom MS, Angeles TS, Breslin HJ, Gingrich DE, Huang Z, Lisko JG, Mason JL, Milkiewicz KL, Thieu TV, Underiner TL, Wells GJ, Wells-Knecht KJ, Dorsey BD.
Bioorg Med Chem Lett (2011) 21 : 7325 -7330
PubMed 22041060 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.79 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1822525 1 8.05
CHEMBL1923569 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1822525 IC50 = 9.0 nM 8.05
CHEMBL1923569 IC50 = 30.0 nM 7.52