Assay Detail

CHEMBL2389433

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Binding

Inhibition of human JAK1 (837-1142) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay

ChEMBL ↗

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Target

Tyrosine-protein kinase JAK1 (CHEMBL2835) ↗

Open DB target context

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Tyrosine-protein kinase JAK1 (CHEMBL2835) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase JAK1

CHEMBL2835

Anchored from Assay target.

Protein identity Tyrosine-protein kinase JAK1

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 JAK1 (CHEMBL2835) ↗

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	9.70	9.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1789941	RUXOLITINIB	4.0	1	9.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1789941	RUXOLITINIB	Ki	=	0.2	nM	9.70