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Assay Detail

CHEMBL5255776

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

Binding
Inhibition of TYK2 dependent IFNalpha-stimulated STAT3 phosphorylation in human Jurkat cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel N-(methyl-d<sub>3</sub>) pyridazine-3-carboxamide derivatives as TYK2 inhibitors.
Liu F, Wang B, Liu Y, Shi W, Hu Z, Chang X, Tang X, Zhang Y, Xu H, He Y.
Bioorg Med Chem Lett (2023) 86 : 129235 -129235
PubMed 36907336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.20 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5273814 1 9.09
CHEMBL5282623 1 9.00
CHEMBL5268371 1 8.85
CHEMBL5286565 1 8.74
CHEMBL5267449 1 8.72
CHEMBL5281991 1 8.60
CHEMBL5270922 1 8.51
CHEMBL5284638 1 8.49
CHEMBL4435170 DEUCRAVACITINIB 4.0 1 8.34
CHEMBL5279644 1 8.32
CHEMBL5270823 1 8.24
CHEMBL5278999 1 8.19
CHEMBL5280466 1 8.08
CHEMBL5285091 1 8.00
CHEMBL5278635 1 7.96
CHEMBL5273136 1 7.92
CHEMBL5266772 1 7.89
CHEMBL5269164 1 7.85
CHEMBL5291007 1 7.62
CHEMBL5282377 1 7.37
CHEMBL5284232 1 7.29
CHEMBL5289104 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5273814 IC50 = 0.81 nM 9.09
CHEMBL5282623 IC50 = 1.0 nM 9.00
CHEMBL5268371 IC50 = 1.4 nM 8.85
CHEMBL5286565 IC50 = 1.8 nM 8.74
CHEMBL5267449 IC50 = 1.9 nM 8.72
CHEMBL5281991 IC50 = 2.5 nM 8.60
CHEMBL5270922 IC50 = 3.1 nM 8.51
CHEMBL5284638 IC50 = 3.2 nM 8.49
CHEMBL4435170 DEUCRAVACITINIB IC50 = 4.6 nM 8.34
CHEMBL5279644 IC50 = 4.8 nM 8.32
CHEMBL5270823 IC50 = 5.7 nM 8.24
CHEMBL5278999 IC50 = 6.4 nM 8.19
CHEMBL5280466 IC50 = 8.3 nM 8.08
CHEMBL5285091 IC50 = 10.0 nM 8.00
CHEMBL5278635 IC50 = 11.0 nM 7.96
CHEMBL5273136 IC50 = 12.0 nM 7.92
CHEMBL5266772 IC50 = 13.0 nM 7.89
CHEMBL5269164 IC50 = 14.0 nM 7.85
CHEMBL5291007 IC50 = 24.0 nM 7.62
CHEMBL5282377 IC50 = 43.0 nM 7.37
CHEMBL5284232 IC50 = 51.0 nM 7.29
CHEMBL5289104 IC50 = 55.0 nM 7.26