Assay Detail

CHEMBL2155754

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Binding

Inhibition of human recombinant JAK3 kinase domain using FITC-KGGEEEEYFELVKK as substrate by peptide mobility shift assay

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
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL2148) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.

Kulagowski JJ, Blair W, Bull RJ, Chang C, Deshmukh G, Dyke HJ, Eigenbrot C, Ghilardi N, Gibbons P, Harrison TK, Hewitt PR, Liimatta M, Hurley CA, Johnson A, Johnson T, Kenny JR, Bir Kohli P, Maxey RJ, Mendonca R, Mortara K, Murray J, Narukulla R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Waszkowycz B, Zak M.
J Med Chem (2012) 55 : 5901 -5921
PubMed 22591402 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	9.62	9.62

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL221959	TOFACITINIB	4.0	1	9.62

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL221959	TOFACITINIB	Ki	=	0.24	nM	9.62