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Assay Detail

CHEMBL2329029

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

Binding
Inhibition of JAK1/JAK2/TYK2 in C57BL/6 mouse whole blood assessed as inhibition of IL-6-stimulated STAT3 phosphorylation after 30 mins by flow cytometric analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Blood
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

TYK2/JAK1/JAK2 (CHEMBL3885642)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
Soth M, Hermann JC, Yee C, Alam M, Barnett JW, Berry P, Browner MF, Frank K, Frauchiger S, Harris S, He Y, Hekmat-Nejad M, Hendricks T, Henningsen R, Hilgenkamp R, Ho H, Hoffman A, Hsu PY, Hu DQ, Itano A, Jaime-Figueroa S, Jahangir A, Jin S, Kuglstatter A, Kutach AK, Liao C, Lynch S, Menke J, Niu L, Patel V, Railkar A, Roy D, Shao A, Shaw D, Steiner S, Sun Y, Tan SL, Wang S, Vu MD.
J Med Chem (2013) 56 : 345 -356
PubMed 23214979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.49 5.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221959 TOFACITINIB 4.0 1 5.76
CHEMBL2325898 1 5.70
CHEMBL2325895 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221959 TOFACITINIB IC50 = 1720.0 nM 5.76
CHEMBL2325898 IC50 = 2010.0 nM 5.70
CHEMBL2325895 IC50 = 9900.0 nM 5.00