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Assay Detail

CHEMBL4258467

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

Binding
Inhibition of human JAK3 using GGEEEEYFELVKKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method
3
Total Activities
3
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

Tyrosine-protein kinase JAK3 (CHEMBL2148)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and evaluation of (<i>R</i>)-3-(7-(methyl(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.
Chough C, Lee S, Joung M, Lee J, Kim JH, Kim BM.
Medchemcomm (2018) 9 : 477 -489
PubMed 30108938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.34 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4293578 1 6.96
CHEMBL3301607 FILGOTINIB 4.0 1 6.09
CHEMBL4279819 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4293578 IC50 = 110.0 nM 6.96
CHEMBL3301607 FILGOTINIB IC50 = 810.0 nM 6.09
CHEMBL4279819 IC50 = 1100.0 nM 5.96