JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules Article Swipe
Ana S. Newton
,
Luca Deiana
,
D.E. Puleo
,
José A. Cisneros
,
Kara J. Cutrona
,
Joseph Schlessinger
,
William L. Jorgensen
·
YOU?
·
· 2017
· Open Access
·
· DOI: https://doi.org/10.1021/acsmedchemlett.7b00154
YOU?
·
· 2017
· Open Access
·
· DOI: https://doi.org/10.1021/acsmedchemlett.7b00154
A competitive fluorescence polarization (FP) assay is reported for determining binding affinities of probe molecules with the pseudokinase JAK2 JH2 allosteric site. The syntheses of the fluorescent 5 and 6 used in the assay are reported as well as Kd results for 10 compounds, including JNJ7706621, NVP-BSK805, and filgotinib (GLPG0634). X-ray crystal structures of JAK2 JH2 in complex with NVP-BSK805, filgotinib, and diaminopyrimidine 8 elucidate the binding poses.
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- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1021/acsmedchemlett.7b00154
- OA Status
- green
- Cited By
- 28
- References
- 23
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W2615057371
All OpenAlex metadata
Raw OpenAlex JSON
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https://openalex.org/W2615057371Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.1021/acsmedchemlett.7b00154Digital Object Identifier
- Title
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JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small MoleculesWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2017Year of publication
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2017-05-17Full publication date if available
- Authors
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Ana S. Newton, Luca Deiana, D.E. Puleo, José A. Cisneros, Kara J. Cutrona, Joseph Schlessinger, William L. JorgensenList of authors in order
- Landing page
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https://doi.org/10.1021/acsmedchemlett.7b00154Publisher landing page
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YesWhether a free full text is available
- OA status
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greenOpen access status per OpenAlex
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https://doi.org/10.7270/q2f76fz8Direct OA link when available
- Concepts
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Fluorescence, Fluorescence anisotropy, Allosteric regulation, Molecule, Chemistry, Small molecule, Affinities, Stereochemistry, Crystal structure, Crystallography, Biochemistry, Receptor, Organic chemistry, Quantum mechanics, PhysicsTop concepts (fields/topics) attached by OpenAlex
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28Total citation count in OpenAlex
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2025: 1, 2024: 2, 2023: 2, 2022: 6, 2021: 5Per-year citation counts (last 5 years)
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23Number of works referenced by this work
- Related works (count)
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10Other works algorithmically related by OpenAlex
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