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Assay Detail

CHEMBL4414860

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Binding
Inhibition of human ERG by patch clamp assay
2
Total Activities
2
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

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 2 5.60 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4526283 1 5.60
CHEMBL4444178 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4526283 IC50 = 2500.0 nM 5.60
CHEMBL4444178 IC50 > 30000.0 nM -