Assay Detail

CHEMBL2160362

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Binding

Inhibition of JAK3 kinase domain using N-terminal 5-carboxyfluorescein-tagged Leu-Pro-Leu-Asp-Lys-Asp-Tyr-Tyr-Val-Val-Arg as substrate after 30 mins

ChEMBL ↗

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Target

Tyrosine-protein kinase JAK3 (CHEMBL2148) ↗

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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
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL2148) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y.
J Med Chem (2012) 55 : 6176 -6193
PubMed 22698084 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	8.08	8.49

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1789941	RUXOLITINIB	4.0	1	8.49
CHEMBL2159210	—	—	1	7.66

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1789941	RUXOLITINIB	Ki	=	3.2	nM	8.49
CHEMBL2159210	—	Ki	=	22.0	nM	7.66