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Assay Detail

CHEMBL5319087

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

Binding
Inhibition of JAK1/JAK3 in human M07E cells assessed as reduction of IL-15 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-15 stimulation and measured after 15 mins by flow cytometry analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type M07E
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

JAK3/JAK1 (CHEMBL3038491)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Thoma G, Duthaler RO, Waelchli R, Hauchard A, Bruno S, Strittmatter-Keller U, Orjuela Leon A, Viebrock S, Aichholz R, Beltz K, Grove K, Hoque S, Rudewicz PJ, Zerwes HG.
J Med Chem (2023) 66 : 2161 -2168
PubMed 36657024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.54 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105759 BARICITINIB 4.0 1 8.30
CHEMBL4297507 DELGOCITINIB 3.0 1 8.05
CHEMBL3622821 UPADACITINIB 4.0 1 7.89
CHEMBL1789941 RUXOLITINIB 4.0 1 7.75
CHEMBL221959 TOFACITINIB 4.0 1 7.66
CHEMBL5403330 1 7.39
CHEMBL5409666 1 7.35
CHEMBL3655081 ABROCITINIB 4.0 1 7.33
CHEMBL4747591 1 7.27
CHEMBL5270549 1 7.27
CHEMBL5433426 1 7.18
CHEMBL5415586 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105759 BARICITINIB IC50 = 5.0 nM 8.30
CHEMBL4297507 DELGOCITINIB IC50 = 9.0 nM 8.05
CHEMBL3622821 UPADACITINIB IC50 = 13.0 nM 7.89
CHEMBL1789941 RUXOLITINIB IC50 = 18.0 nM 7.75
CHEMBL221959 TOFACITINIB IC50 = 22.0 nM 7.66
CHEMBL5403330 IC50 = 41.0 nM 7.39
CHEMBL5409666 IC50 = 45.0 nM 7.35
CHEMBL3655081 ABROCITINIB IC50 = 47.0 nM 7.33
CHEMBL4747591 IC50 = 54.0 nM 7.27
CHEMBL5270549 IC50 = 54.0 nM 7.27
CHEMBL5433426 IC50 = 66.0 nM 7.18
CHEMBL5415586 IC50 = 85.0 nM 7.07