Assay Detail

CHEMBL1108564

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Binding

Inhibition of JAK2 V617F mutant (JH1-JH2)

ChEMBL ↗

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Target

Tyrosine-protein kinase JAK2 (CHEMBL2971) ↗

Open DB target context

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Tyrosine-protein kinase JAK2 (CHEMBL2971) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase JAK2

CHEMBL2971

Anchored from Assay target.

Protein identity Tyrosine-protein kinase JAK2

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 JAK2 (CHEMBL2971) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).

Burns CJ, Bourke DG, Andrau L, Bu X, Charman SA, Donohue AC, Fantino E, Farrugia M, Feutrill JT, Joffe M, Kling MR, Kurek M, Nero TL, Nguyen T, Palmer JT, Phillips I, Shackleford DM, Sikanyika H, Styles M, Su S, Treutlein H, Zeng J, Wilks AF.
Bioorg Med Chem Lett (2009) 19 : 5887 -5892
PubMed 19762238 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.96	7.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1078178	MOMELOTINIB	4.0	1	7.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1078178	MOMELOTINIB	IC50	=	11.0	nM	7.96