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Assay Detail

CHEMBL5329059

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

Binding
Inhibition of JAK1 (unknown origin) in presence of Mg/ATP mixture by [gamma p33]-ATP based radiometric assay
8
Total Activities
8
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 JAK1 (CHEMBL2835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of <i>N</i>-(4-(Aminomethyl)phenyl)-5-methylpyrimidin-2-amine Derivatives as Potent and Selective JAK2 Inhibitors.
Tian Y, Qin S, Zhang F, Luo J, He X, Sun Y, Yang T.
ACS Med Chem Lett (2023) 14 : 1113 -1121
PubMed 37583815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.03 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4753549 1 7.38
CHEMBL5403283 1 7.37
CHEMBL5440964 1 7.14
CHEMBL5408994 1 7.06
CHEMBL5432626 1 6.97
CHEMBL5424098 1 6.85
CHEMBL5419978 1 6.75
CHEMBL5422938 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4753549 IC50 = 42.0 nM 7.38
CHEMBL5403283 IC50 = 43.0 nM 7.37
CHEMBL5440964 IC50 = 73.0 nM 7.14
CHEMBL5408994 IC50 = 87.0 nM 7.06
CHEMBL5432626 IC50 = 106.0 nM 6.97
CHEMBL5424098 IC50 = 142.0 nM 6.85
CHEMBL5419978 IC50 = 178.0 nM 6.75
CHEMBL5422938 IC50 = 193.0 nM 6.71