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Assay Detail

CHEMBL4414854

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

Binding
Inhibition of TYK2 JH2 (unknown origin) by morrison titration assay
3
Total Activities
3
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

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

Publication

Identification of <i>N</i>-Methyl Nicotinamide and <i>N</i>-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).
Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS.
J Med Chem (2019) 62 : 8953 -8972
PubMed 31314518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.82 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4561663 1 10.22
CHEMBL4440718 1 10.15
CHEMBL4444178 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4561663 Ki = 0.06 nM 10.22
CHEMBL4440718 Ki = 0.07 nM 10.15
CHEMBL4444178 Ki = 0.8 nM 9.10