Assay Detail

CHEMBL4377472

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Binding

Allosteric inhibition of fluorescein labeled probe binding to His-tagged recombinant human TYK2 pseudokinase JH2 domain (575-869 residues) incubated for 1 hr by HTRF assay

ChEMBL ↗

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Target

Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗

Open DB target context

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Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Non-receptor tyrosine-protein kinase TYK2

CHEMBL3553

Anchored from Assay target.

Protein identity Non-receptor tyrosine-protein kinase TYK2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS.
J Med Chem (2019) 62 : 8973 -8995
PubMed 31318208 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.70	9.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4435170	DEUCRAVACITINIB	4.0	1	9.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4435170	DEUCRAVACITINIB	IC50	=	0.2	nM	9.70