Determination of Ligand-Binding Affinity (


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
10 08 2023
Historique:
medline: 11 8 2023
pubmed: 19 7 2023
entrez: 19 7 2023
Statut: ppublish

Résumé

High hit rates from initial ligand-observed NMR screening can make it challenging to prioritize which hits to follow up, especially in cases where there are no available crystal structures of these hits bound to the target proteins or other strategies to provide affinity ranking. Here, we report a reproducible, accurate, and versatile quantitative ligand-observed NMR assay, which can determine

Identifiants

pubmed: 37467168
doi: 10.1021/acs.jmedchem.3c00758
pmc: PMC10424183
doi:

Substances chimiques

Ligands 0
Small Molecule Libraries 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

10617-10627

Subventions

Organisme : Cancer Research UK
ID : C309/A11566
Pays : United Kingdom

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Auteurs

Manjuan Liu (M)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Amin Mirza (A)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

P Craig McAndrew (PC)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Arjun Thapaliya (A)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Olivier A Pierrat (OA)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Mark Stubbs (M)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Tamas Hahner (T)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Nicola E A Chessum (NEA)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Paolo Innocenti (P)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

John Caldwell (J)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Matthew D Cheeseman (MD)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Benjamin R Bellenie (BR)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Rob L M van Montfort (RLM)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K.

Gary K Newton (GK)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Rosemary Burke (R)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Ian Collins (I)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

Swen Hoelder (S)

Centre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.

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Classifications MeSH