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Assay Detail

CHEMBL2186603

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

Binding
Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type TF-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP.
J Med Chem (2012) 55 : 10090 -10107
PubMed 23061660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.51 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1789941 RUXOLITINIB 4.0 1 8.16
CHEMBL2178804 1 8.13
CHEMBL2178805 1 8.01
CHEMBL2178801 1 7.65
CHEMBL2178800 1 7.46
CHEMBL2178803 1 7.39
CHEMBL2178799 1 7.37
CHEMBL2178266 1 7.19
CHEMBL2178802 1 7.16
CHEMBL2177122 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1789941 RUXOLITINIB IC50 = 6.85 nM 8.16
CHEMBL2178804 IC50 = 7.4 nM 8.13
CHEMBL2178805 IC50 = 9.8 nM 8.01
CHEMBL2178801 IC50 = 22.4 nM 7.65
CHEMBL2178800 IC50 = 34.5 nM 7.46
CHEMBL2178803 IC50 = 40.4 nM 7.39
CHEMBL2178799 IC50 = 42.3 nM 7.37
CHEMBL2178266 IC50 = 64.2 nM 7.19
CHEMBL2178802 IC50 = 68.6 nM 7.16
CHEMBL2177122 IC50 = 242.0 nM 6.62