Assay Detail

CHEMBL2389439

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Binding

Inhibition of human GST-fused JAK3 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA

ChEMBL ↗

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Target

Tyrosine-protein kinase JAK3 (CHEMBL2148) ↗

Open DB target context

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Tyrosine-protein kinase JAK3 (CHEMBL2148) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase JAK3

CHEMBL2148

Anchored from Assay target.

Protein identity Tyrosine-protein kinase JAK3

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
Cell Type	Sf9
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL2148) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.

Liang J, van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair W, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, Kohli PB, Lai Y, Liu Y, Lyssikatos J, Mantik P, Menghrajani K, Murray J, Peng I, Sambrone A, Shia S, Shin Y, Smith J, Sohn S, Tsui V, Ultsch M, Wu LC, Xiao Y, Yang W, Young J, Zhang B, Zhu BY, Magnuson S.
J Med Chem (2013) 56 : 4521 -4536
PubMed 23668484 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	9.40	9.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL221959	TOFACITINIB	4.0	1	9.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL221959	TOFACITINIB	Ki	=	0.4	nM	9.40