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Assay Detail

CHEMBL5327941

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

Functional
In vivo inhibition of JAK/STAT signaling pathway in mouse assessed as downregulation of IFN-gamma induced CXCL10 gene expression in whole blood treated sc followed by 24 hrs blood collected and measured by RT-PCR analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613561)
Type TISSUE
Organism Mus musculus

Publication

Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
Leit S, Greenwood J, Carriero S, Mondal S, Abel R, Ashwell M, Blanchette H, Boyles NA, Cartwright M, Collis A, Feng S, Ghanakota P, Harriman GC, Hosagrahara V, Kaila N, Kapeller R, Rafi SB, Romero DL, Tarantino PM, Timaniya J, Toms AV, Wester RT, Westlin W, Srivastava B, Miao W, Tummino P, McElwee JJ, Edmondson SD, Masse CE.
J Med Chem (2023) 66 : 10473 -10496
PubMed 37427891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.27 6.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5430689 1 6.59
CHEMBL5422616 1 6.46
CHEMBL5418744 1 6.43
CHEMBL5405569 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5430689 IC50 = 254.0 nM 6.59
CHEMBL5422616 IC50 = 347.0 nM 6.46
CHEMBL5418744 IC50 = 372.0 nM 6.43
CHEMBL5405569 IC50 = 2640.0 nM 5.58