Assay Detail

CHEMBL3625653

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Binding

Binding affinity to JAK2 (unknown origin) assessed as dissociation constant

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

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV.
ACS Med Chem Lett (2015) 6 : 850 -855
PubMed 26288683 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	1	9.32	9.32

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3545215	BMS-911543	2.0	1	9.32

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3545215	BMS-911543	Kd	=	0.48	nM	9.32