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Assay Detail

CHEMBL3766658

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

Binding
Inhibition of TYK2/JAK2 in human PBMC assessed as reduction in IL-23-induced STAT4 phosphorylation preincubated for 5 mins followed by IL-23 stimulation for 15 to 60 mins by flow cytometry analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

JAK2/TYK2 (CHEMBL3301392)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.
Yogo T, Nagamiya H, Seto M, Sasaki S, Shih-Chung H, Ohba Y, Tokunaga N, Lee GN, Rhim CY, Yoon CH, Cho SY, Skene R, Yamamoto S, Satou Y, Kuno M, Miyazaki T, Nakagawa H, Okabe A, Marui S, Aso K, Yoshida M.
J Med Chem (2016) 59 : 733 -749
PubMed 26701356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.67 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105759 BARICITINIB 4.0 1 6.70
CHEMBL3765822 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105759 BARICITINIB IC50 = 200.0 nM 6.70
CHEMBL3765822 IC50 = 230.0 nM 6.64