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Assay Detail

CHEMBL2214768

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

Functional
Inhibition of JAK2 in HEL 92.1.7 cells xenografted in po dosed nude mouse assessed as inhibition of STAT3 phosphorylation after 4 hrs
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEL
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P.
Bioorg Med Chem Lett (2012) 22 : 7653 -7658
PubMed 23127890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.89 4.89
ED50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2208034 2 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2208034 IC50 = 13000.0 nM 4.89
CHEMBL2208034 ED50 = 210.0 mg.kg-1 -