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Assay Detail

CHEMBL5329055

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

Binding
Inhibition of JAK2 V617F mutant in mouse BaF3 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL1649049)
Type SINGLE PROTEIN
Organism Mus musculus

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 19 6.70 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5422938 1 7.60
CHEMBL4753549 1 7.39
CHEMBL5419978 1 7.27
CHEMBL5424098 1 7.16
CHEMBL5408994 1 7.14
CHEMBL5403283 1 7.06
CHEMBL5440964 1 7.01
CHEMBL5408539 1 7.00
CHEMBL5432626 1 6.89
CHEMBL5404973 1 6.77
CHEMBL5437784 1 6.75
CHEMBL5429688 1 6.74
CHEMBL5436902 1 6.58
CHEMBL5418281 1 6.43
CHEMBL5416914 1 6.42
CHEMBL5415635 1 6.06
CHEMBL5398984 1 5.94
CHEMBL5429799 1 5.66
CHEMBL5416946 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5422938 IC50 = 25.3 nM 7.60
CHEMBL4753549 IC50 = 41.0 nM 7.39
CHEMBL5419978 IC50 = 53.3 nM 7.27
CHEMBL5424098 IC50 = 69.2 nM 7.16
CHEMBL5408994 IC50 = 72.0 nM 7.14
CHEMBL5403283 IC50 = 87.5 nM 7.06
CHEMBL5440964 IC50 = 98.1 nM 7.01
CHEMBL5408539 IC50 = 101.1 nM 7.00
CHEMBL5432626 IC50 = 129.2 nM 6.89
CHEMBL5404973 IC50 = 169.5 nM 6.77
CHEMBL5437784 IC50 = 178.3 nM 6.75
CHEMBL5429688 IC50 = 182.4 nM 6.74
CHEMBL5436902 IC50 = 265.5 nM 6.58
CHEMBL5418281 IC50 = 371.9 nM 6.43
CHEMBL5416914 IC50 = 384.6 nM 6.42
CHEMBL5415635 IC50 = 869.5 nM 6.06
CHEMBL5398984 IC50 = 1139.5 nM 5.94
CHEMBL5429799 IC50 = 2204.4 nM 5.66
CHEMBL5416946 IC50 = 3314.5 nM 5.48