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Assay Detail

CHEMBL3388144

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

Binding
Inhibition of human recombinant JAK2
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 JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L.
J Med Chem (2014) 57 : 9323 -9342
PubMed 25369270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.59 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1789941 RUXOLITINIB 4.0 1 9.70
CHEMBL221959 TOFACITINIB 4.0 1 9.22
CHEMBL3360318 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1789941 RUXOLITINIB IC50 = 0.2 nM 9.70
CHEMBL221959 TOFACITINIB IC50 = 0.6 nM 9.22
CHEMBL3360318 IC50 = 138.0 nM 6.86