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Assay Detail

CHEMBL4414786

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

Binding
Inhibition of TYK2 JH1 domain (unknown origin)
10
Total Activities
10
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
IC50 10 6.50 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4561663 1 7.82
CHEMBL4530719 1 7.38
CHEMBL4444178 1 4.30
CHEMBL4537678 1 -
CHEMBL4559521 1 -
CHEMBL4466720 1 -
CHEMBL4516272 1 -
CHEMBL4526283 1 -
CHEMBL4444169 1 -
CHEMBL4440718 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4561663 IC50 = 15.0 nM 7.82
CHEMBL4530719 IC50 = 42.0 nM 7.38
CHEMBL4444178 IC50 = 50000.0 nM 4.30
CHEMBL4537678 IC50 > 2000.0 nM -
CHEMBL4559521 IC50 > 2000.0 nM -
CHEMBL4466720 IC50 > 2000.0 nM -
CHEMBL4516272 IC50 > 2000.0 nM -
CHEMBL4526283 IC50 > 50000.0 nM -
CHEMBL4444169 IC50 > 50000.0 nM -
CHEMBL4440718 IC50 > 50000.0 nM -