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Assay Detail

CHEMBL5319084

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

Binding
Inhibition of JAK2 JH1 domain (unknown origin) using Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
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 7.73 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105759 BARICITINIB 4.0 1 8.54
CHEMBL3622821 UPADACITINIB 4.0 1 8.51
CHEMBL1789941 RUXOLITINIB 4.0 1 8.40
CHEMBL5409666 1 8.10
CHEMBL5415586 1 7.85
CHEMBL221959 TOFACITINIB 4.0 1 7.58
CHEMBL4747591 1 7.58
CHEMBL5403330 1 7.57
CHEMBL5433426 1 7.54
CHEMBL4297507 DELGOCITINIB 3.0 1 7.43
CHEMBL5270549 1 7.32
CHEMBL3655081 ABROCITINIB 4.0 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105759 BARICITINIB IC50 = 2.9 nM 8.54
CHEMBL3622821 UPADACITINIB IC50 = 3.1 nM 8.51
CHEMBL1789941 RUXOLITINIB IC50 = 4.0 nM 8.40
CHEMBL5409666 IC50 = 8.0 nM 8.10
CHEMBL5415586 IC50 = 14.0 nM 7.85
CHEMBL221959 TOFACITINIB IC50 = 26.0 nM 7.58
CHEMBL4747591 IC50 = 26.0 nM 7.58
CHEMBL5403330 IC50 = 27.0 nM 7.57
CHEMBL5433426 IC50 = 29.0 nM 7.54
CHEMBL4297507 DELGOCITINIB IC50 = 37.0 nM 7.43
CHEMBL5270549 IC50 = 48.0 nM 7.32
CHEMBL3655081 ABROCITINIB IC50 = 412.0 nM 6.38